Tridal Liquid

Pronunciation: KOE-deen/gwye-FEN-e-sin/fen-ill-EF-rin
Generic Name: Codeine/Guaifenesin/Phenylephrine
Brand Name: Giltuss Ped-C and Tridal

Tridal Liquid is used for:

Relieving congestion, cough, and throat and airway irritation due to colds, flu, or hay fever. It may also be used for other conditions as determined by your doctor.

Tridal Liquid is a decongestant, cough suppressant, and expectorant combination. It works by constricting blood vessels and reducing swelling in the nasal passages, loosening mucus and lung secretions in the chest, and making coughs more productive. The cough suppressant works in the brain to help decrease the cough reflex to reduce a dry cough.

Do NOT use Tridal Liquid if:

• you are allergic to any ingredient in Tridal Liquid or any other codeine or morphine related medicine (eg, oxycodone)


• you have severe high blood pressure, rapid heartbeat, or other severe heart problems (eg, heart blood vessel disease)


• you are taking sodium oxybate (GHB) or you have taken furazolidone or a monoamine oxidase (MAO) inhibitor (eg, phenelzine) within the last 14 days

Contact your doctor or health care provider right away if any of these apply to you.

Before using Tridal Liquid:

Some medical conditions may interact with Tridal Liquid. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have had a severe allergic reaction (eg, severe rash, hives, difficulty breathing, dizziness) to morphine, codeine, or any other opiate (eg, hydrocodone, dihydrocodeine, oxycodone)


• if you have a history of glaucoma, an enlarged prostate gland or other prostate problems, heart problems, diabetes, high blood pressure, blood vessel problems, stroke, kidney or liver problems, a blockage of your bowel or bladder, adrenal gland problems (eg, Addison disease), or an underactive thyroid


• if you have a history of stomach problems, bowel problems (eg, chronic inflammation or ulceration of the bowel), or gallbladder problems (eg, gallstones), or if you have had recent abdominal surgery


• if you have a history of asthma, chronic cough, lung problems (eg, chronic bronchitis, emphysema), or chronic obstructive pulmonary disease (COPD), or if your cough occurs with large amounts of mucus


• if you have recently had any head injury, brain injury or tumor, increased pressure in the brain, infection of the brain or nervous system, epilepsy, or seizures


• if you have a history of alcohol abuse, drug abuse, or suicidal thoughts or behavior

Some MEDICINES MAY INTERACT with Tridal Liquid. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Beta-blockers (eg, propranolol), catechol-O-methyltransferase (COMT) inhibitors (eg, tolcapone), cimetidine, furazolidone, HIV protease inhibitors (eg, ritonavir), indomethacin, MAO inhibitors (eg, phenelzine), or tricyclic antidepressants (eg, amitriptyline) because the risk of side effects from Tridal Liquid may be increased


• Digoxin, droxidopa, or sodium oxybate (GHB) because the risk of severe drowsiness, breathing problems, seizures, irregular heartbeat, or heart attack may be increased


• Naltrexone and quinidine because the effectiveness of Tridal Liquid may be decreased.


• Bromocriptine because the risk of side effects may be increased by Tridal Liquid


• Guanadrel, guanethidine, mecamylamine, methyldopa, or reserpine because effectiveness may be decreased by Tridal Liquid

This may not be a complete list of all interactions that may occur. Ask your health care provider if Tridal Liquid may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Tridal Liquid:

Use Tridal Liquid as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Take Tridal Liquid by mouth with or without food.


• Drink plenty of water while taking Tridal Liquid.


• Use a measuring device marked for medicine dosing. Ask your pharmacist for help if you are unsure of how to measure your dose.


• If you miss a dose of Tridal Liquid, take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Tridal Liquid.

Important safety information:

• Tridal Liquid may cause dizziness or drowsiness. These effects may be worse if you take it with alcohol or certain medicines. Use Tridal Liquid with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Do not take appetite suppressants while you are taking Tridal Liquid without checking with your doctor.


• Tridal Liquid has phenylephrine in it. Before you start any new medicine, check the label to see if it has phenylephrine in it too. If it does or if you are not sure, check with your doctor or pharmacist.


• Do NOT take more than the recommended dose or use for longer than prescribed without checking with your doctor.


• If your symptoms do not get better within 5 to 7 days or if they get worse, check with your doctor.


• Tridal Liquid may interfere with certain lab tests. Be sure your doctor and lab personnel know you are taking Tridal Liquid.


• Tell your doctor or dentist that you take Tridal Liquid before you receive any medical or dental care, emergency care, or surgery.


• Use Tridal Liquid with caution in the ELDERLY; they may be more sensitive to its effects.


• Caution is advised when using Tridal Liquid in CHILDREN; they may be more sensitive to its effects.


• PREGNANCY and BREAST-FEEDING: If you become pregnant, contact your doctor. You will need to discuss the benefits and risks of using Tridal Liquid while you are pregnant. It is not known if Tridal Liquid is found in breast milk. Do not breast-feed while taking Tridal Liquid.

Possible side effects of Tridal Liquid:

All medicines may cause side effects, but many people have no, or minor side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Dizziness; drowsiness; excitability; headache; nausea; nervousness or anxiety; trouble sleeping; weakness.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); difficulty urinating; fast or irregular heartbeat; hallucinations; seizures; severe dizziness, lightheadedness, or headache; severe drowsiness; tremor.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Tridal side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately. Symptoms may include blurred vision; confusion; hallucinations; seizures; severe dizziness, lightheadedness, or headache; severe drowsiness; unusually fast, slow, or irregular heartbeat; vomiting.

Proper storage of Tridal Liquid:

Store Tridal Liquid at room temperature, between 59 and 86 degrees F (15 and 30 degrees C). Store away from heat, moisture, and light. Do not store in the bathroom. Keep Tridal Liquid out of the reach of children and away from pets.

General information:

• If you have any questions about Tridal Liquid, please talk with your doctor, pharmacist, or other health care provider.


• Tridal Liquid is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Tridal Liquid. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Tridal resources

• Tridal Side Effects (in more detail)
• Tridal Use in Pregnancy & Breastfeeding
• Tridal Drug Interactions
• Tridal Support Group
• 0 Reviews for Tridal - Add your own review/rating

Compare Tridal with other medications

• Cough and Nasal Congestion

Pariet 10mg & 20mg

Pariet 20 mg

Pariet 10 mg

Please read this leaflet carefully before you start to use your medicine. It contains a summary of the information available on your medicine. If after reading this you do not understand or have any questions, ask your doctor or pharmacist (chemist).

Pharmaceutical companies are not allowed to answer questions from patients about their medicines.

Keep this leaflet. You may want to read it again.

About your medicine

Trade Name

The name of your medicine is

PARIET 20mg or

PARIET 10mg.

Composition

What is the active substance?

The active ingredient is rabeprazole sodium.

Each yellow PARIET tablet contains 20mg rabeprazole sodium; and each pink PARIET tablet contains 10mg of rabeprazole sodium.

The tablets also contain the following inactive ingredients: mannitol, magnesium oxide, low substituted hyprolose, hyprolose, magnesium stearate, ethylcellulose, hypromellose phthalate, diacetylated monoglycerides, talc, titanium dioxide (E171), yellow iron oxide (E172) (20mg only), red iron oxide (E172) (10mg only), carnauba wax and ink ((White shellac, red iron oxide (E172), Carnauba wax, Glycerine fatty acid ester, Dehydrated Ethyl Alcohol, 1-Butanol - 20mg tablets); and (White shellac, black iron oxide (E172), Dehydrated Ethyl Alcohol, 1-Butanol - 10mg tablets)).

Pharmaceutical form and treatment classification

What is PARIET (rabeprazole sodium)?

PARIET (rabeprazole sodium) belongs to a class of medicines called Proton Pump Inhibitors (PPIs).

PARIET is available as yellow or pink enteric-coated delayed-release (gastro-resistant) tablets.

The tablets come in aluminium foil blister strips of 1, 7, 10, 14 or 15 tablets per strip. Multiples of these blister strips are placed directly into a carton.

Marketing and manufacturing of PARIET

Who is the Marketing Authorisation Holder responsible for PARIET?

The name and address of the company holding the Product Licence for PARIET is:

Eisai Ltd.

Hammersmith International Centre

3 Shortlands

London

W6 8EE

UK

Who is responsible for manufacturing PARIET?

Eisai Ltd.

Hammersmith International Centre

3 Shortlands

London

W6 8EE

UK

PARIET bulk tablets are manufactured for Eisai Ltd. by:

Eisai Co. Ltd.

(Misato Plant)

950 Oaza Hiroki

Misato-cho

Kodama-gun

Saitama Prefecture 367-0198

Japan

What your medicine is for

Why take PARIET tablets?

PARIET tablets are used to treat people diagnosed as having active duodenal ulcer, active benign gastric/stomach ulcer (peptic ulcers), symptomatic erosive or ulcerative gastro-oesophageal reflux disease (GORD) commonly referred to as inflammation of the gullet caused by acid and associated with heartburn, or for long-term treatment of GORD (GORD maintenance). PARIET tablets are also used for the symptomatic treatment of moderate to very severe gastrooesophageal reflux disease (symptomatic GORD) also associated with heartburn.

PARIET tablets act by reducing the amount of acid made by the stomach. This allows ulcers to heal and symptoms of pain to improve. Pariet is also sometimes given to patients whose stomachs make extremely high amounts of acid, a condition called Zollinger-Ellison Syndrome. In combination with two antibiotics (clarithromycin and amoxycillin) PARIET tablets are used for the eradication of H pylori infection in patients with peptic ulcer disease. For further information on the antibiotic components of the H pylori eradication therapy see the individual product information leaflets.

PARIET is not recommended for use in children.

Before using PARIET tablets

Do not take this medicine without consulting your doctor.

Tell your doctor or pharmacist if:

• you are allergic to any of the ingredients listed above


• you are allergic to other proton pump inhibitors


• you have been told you have a stomach tumour


• you think you might be pregnant or are breast feeding


• you are under 12 years of age


• you have a history of liver disease


• you are taking either of these medicines, digoxin or ketoconazole


• you are taking any other medicines.

If you are in doubt, consult your doctor or pharmacist before using PARIET tablets.

It is unlikely that PARIET would affect your ability to drive or operate machinery.

However, occasionally rabeprazole sodium can induce drowsiness. Therefore, driving and operating complex machinery should be avoided if this effect occurs during treatment.

How to use PARIET tablets

How much PARIET should you take?

When and how often should you take it?

Always follow your doctor’s or pharmacist’s advice about how and when to take your medicine. Do not change the dose or length of the treatment yourself.

The usual recommended dose you will be prescribed by your doctor for the acute indications - active duodenal ulcer, active benign gastric/stomach ulcer (peptic ulcers), symptomatic erosive or ulcerative gastro-oesophageal reflux disease (GORD) is 20mg; 10mg for the symptomatic treatment of moderate to very severe GORD (symptomatic GORD) and for GORD maintenance 20mg or 10mg to be taken by mouth with a drink of water once each day before eating in the morning.

To treat a condition where your stomach makes extremely high amounts of acid, called Zollinger-Ellison Syndrome, the usual recommended dose you will be prescribed by your doctor is three 20mg tablets once a day to start with. The dose may then be adjusted by your doctor depending on how you respond to the treatment. Your doctor will tell you how many tablets to take and when to take them.

The usual recommended dose you will be prescribed by your doctor for the eradication of H pylori infection is 20mg to be taken (in combination with two antibiotics - clarithromycin 500mg and amoxycillin 1g) twice each day and normally for 7 days.

YOU MUST SWALLOW THE PARIET TABLET WHOLE.

DO NOT CRUSH OR CHEW IT.

For further information on the other components of the H pylori eradication therapy see the individual product information leaflets.

For how long should you take PARIET?

If you have an active duodenal ulcer, your treatment with PARIET is expected to continue for four weeks; but after that time your doctor may decide to continue your treatment for a further four weeks.

If you have an active benign gastric ulcer, your treatment with PARIET is expected to continue for six weeks; but after that time your doctor may decide to continue your treatment for a further six weeks.

If you have erosive or ulcerative gastro-oesophageal reflux disease (GORD), you will be instructed by your doctor or pharmacist to take your PARIET tablet for four to eight weeks. For long-term maintenance treatment of GORD your doctor or pharmacist will advise you on how long to take your tablets.

If you are on long-term treatment you need to see your doctor at regular intervals for review of your tablets and symptoms.

If you have moderate to very severe symptomatic gastro-oesophageal reflux disease (symptomatic GORD), your once daily treatment with PARIET is expected to continue for up to 4 weeks. If your symptoms do not resolve within 4 weeks consult your doctor. Following this initial 4 week treatment, if your symptoms return, your doctor may then tell you to take one PARIET 10mg tablet as and when you require it in order to control your symptoms.

If you have a condition where your stomach makes extremely high amounts of acid, called Zollinger-Ellison Syndrome, your doctor or pharmacist will advise you on how long to take your tablets. If you are on long-term treatment you need to see your doctor at regular intervals for review of your tablets and symptoms.

Your treatment with PARIET (in combination with two antibiotics) for the eradication of H pylori infection will last for 7 days. Relief of symptoms will normally occur before the ulcer has completely healed. Therefore it is important that you do not stop taking the tablets until told to do so by your doctor.

What if you take too many tablets?

Do not take more tablets each day than you are prescribed. If you accidentally take more tablets than the prescribed dose, consult your doctor or the Accident and Emergency Department of your local hospital. Always take the tablets and the carton with you to the hospital so that the doctor knows what has been taken.

What if you miss taking your tablets?

If you forget to take a dose, just take it immediately when you remember, and then continue as usual. If you forget to take your medicine for more than 5 days, call your doctor before taking any more medicine.

How quickly will the treatment start to work?

The clinical trials suggest that pain will start to get better within the first few days after you start taking PARIET. However the time to pain relief may vary from patient to patient.

After using PARIET tablets

What side effects could PARIET cause?

All medicines have some side effects. There have been reports of headaches, diarrhoea, abdominal pain, asthenia (weakness), flatulence (wind), and dry mouth linked with the use of PARIET tablets.

Other effects reported during treatment with PARIET were: rhinitis, pharyngitis, nausea, vomiting, non-specific pain/back/muscle/chest and joint pain, dizziness, flu like syndrome, infection, cough, constipation and insomnia. Further less frequent effects were dyspepsia (indigestion), nervousness, drowsiness, bronchitis, sinusitis, chills, eructation (belching), leg cramps, urinary tract infection, fever, breast swelling, fluid retention and in very isolated cases, anorexia, gastritis, weight gain, kidney problems, depression, itching, vision or taste disturbances, stomatitis (sore mouth), sweating and leucocytosis (increase in white blood cells). In most cases, these have been mild, lasting a short time and resolving without having to stop treatment.

During treatment with PARIET skin rash, redness of the skin, itching and rarely skin blisters, liver problems and acute generalised reactions for example facial swelling, low blood pressure and shortness of breath have been reported which resolve after stopping the treatment.

Rarely, a decrease of white blood cells and/or blood platelets may occur. You should see your doctor immediately if you have any unexplained bruising.

Tell your doctor if you have any of these effects and if they are too uncomfortable for you. Also tell your doctor if any other effects occur while you are taking PARIET tablets.

For further information on the other components of the H pylori eradication therapy see the individual product information leaflets.

How to look after your medicine (PARIET tablets)

How should PARIET tablets be stored?

Do not store this medicine above 25°C.

DO NOT PUT THE TABLETS IN THE REFRIGERATOR.

As with all medicines, PARIET tablets should be kept in a safe place where children cannot see or reach them. This medicine is for you. Only a doctor can prescribe it for you. Do not share it with anyone else. It may harm them, even if they have the same symptoms as you.

DO NOT use PARIET tablets after the expiry date which is shown on the package and blister. Leave your tablets in the blister strip. Only remove one when it is time to take your medicine. If your doctor tells you to stop taking your medicine, you should return any you have not used to your pharmacist who will get rid of them safely.

More information

What can you do to help yourself?

• Peptic ulcer (Duodenal and Gastric ulcers)


• Do’s


• - Do take regular relaxed meals


• - Avoid foods that make you feel bad (or make the symptoms worse).


• Don’ts


• - Don’t take too much alcohol


• - Don’t smoke.


• 
  


• Gastro-oesophageal reflux disease (Oesophagitis)


• Do’s


• - Do squat to pick up objects


• - Do raise the head of your bed on about 20cm blocks


• - Do try to reduce your weight if you are overweight. Avoid foods that make you feel bad (or make the symptoms worse).


• Don’ts


• - Don’t bend over from the waist


• - Don’t sleep lying flat


• - Don’t smoke or wear tight clothing.

The problem of too much acid!

Your doctor has prescribed PARIET tablets in order to treat you for either duodenal ulcer or gastric/stomach ulcer (together called peptic ulcers) or gastro-oesophageal reflux disease commonly referred to as acid inflammation of the gullet or heartburn.

What is a peptic ulcer?

A peptic ulcer is a small area in the stomach or the first part of the small bowel (the duodenum), where the protective lining has been worn away. Peptic ulcers have similarities with other ulcers. Ulcers quite often cause pain.

What causes peptic ulcers?

The stomach joins directly into the duodenum. An ulcer starts when acid normally present in the stomach attacks a small part of the wall of the stomach or duodenum. The stomach is normally covered by a protective coating but ulcers start where this coating is damaged; or, when too much acid from the stomach moves into the duodenum, which has no protective coating. Such ulcers cannot readily heal themselves, where there is continued flow of stomach acid.

What is gastro-oesophageal reflux disease (oesophagitis/GORD)?

Gastro-oesophageal reflux disease (oesophagitis or GORD) is where the oesophagus or gullet becomes inflamed, swollen and ulcerated because of repeated exposure to acid from the stomach.

What causes gastro-oesophageal reflux disease (oesophagitis/GORD)?

The stomach is usually protected from the acid it produces by the protective coating.

But, like the duodenum, the oesophagus has no protective coating. The oesophagus or gullet joins directly to the stomach. When acid from the stomach returns into the gullet, it may become inflamed, swollen and ulcerated. Healing of the inflammation and relief from pain or heartburn can be achieved by reducing the amount of stomach acid.

If you want to know more about your medicine, ask your doctor or pharmacist.

They have more information.

Date PARIET Leaflet (United Kingdom)

last revised: - June 2007

© Copyright Eisai Ltd.

Ref: PA023.1/ZES

Amlodipine 5 mg tablets

1. Name Of The Medicinal Product

Amlodipine 5 mg tablets

2. Qualitative And Quantitative Composition

Each tablet contains Amlodipine besilate equivalent to 5 mg of amlodipine.

For a full list of excipients, see section 6.1.

3. Pharmaceutical Form

Tablet

White or almost white, flat, bevelled edges, barrel-shaped tablet debossed with "C" on one side and "58" on the other side.

4. Clinical Particulars

4.1 Therapeutic Indications

Chronic stable and vasospastic angina pectoris.

Essential hypertension.

4.2 Posology And Method Of Administration

For oral use.

The tablets should be taken with a glass of liquid (e.g. a glass of water) with or without food.

In adults

For the treatment of hypertension and angina pectoris, the starting dose is 5 mg once daily. If the desired therapeutic effect cannot be achieved within 2-4 weeks, the dose can be increased to a maximum of 10 mg daily (given as a single dose) depending on the individual response of the patient. Amlodipine can be used as monotherapy or in combination with anti-anginal medication in patients suffering from angina pectoris.

Children with hypertension from 6 years to 17 years of age

The recommended antihypertensive oral dose in pediatric patients ages 6-17 years is 2.5 mg once daily as a starting dose, up-titrated to 5 mg once daily if blood pressure goal is not achieved after 4 weeks. Doses in excess of 5 mg daily have not been studied in pediatric patients (see section 5.1 and section 5.2). The effect of amlodipine on blood pressure in patients less than 6 years of age is not known

The 2.5 mg dose cannot be obtained with Amlodipine 5 mg tablets as these tablets are not manufactured to break into two equal halves.

Elderly patients

For elderly patients, the normal dose is recommended; however, caution is advised when the dose is increased (see section 5.2).

Patients with renal impairment

The normal dosage is recommended (see section 5.2). Amlodipine is not dialyzable. Amlodipine should be administered with particular caution to patients undergoing dialysis (see section 4.4).

Patients with hepatic impairment

In patients with hepatic impairment, no dosage regimen has been defined, therefore amlodipine should be administered with caution (see section 4.4).

4.3 Contraindications

Amlodipine is contraindicated in patients with:

- hypersensitivity to amlodipine, other dihydropyridines or any of the excipients

- severe hypotension

- shock (including cardiogenic shock)

- obstruction of the outflow tract of the left ventricle (e.g. high grade aortic stenosis)

- haemodynamically unstable heart failure after acute myocardial infarction

4.4 Special Warnings And Precautions For Use

The safety and efficacy of amlodipine in hypertensive crisis has not been established.

Patients with cardiac failure:

Patients with heart failure should be treated with caution. In a long-term, placebo controlled study in patients with severe heart failure (NYHA class III and IV) the reported incidence of pulmonary oedema was higher in the amlodipine treated group than in the placebo group, but this was not associated with worsening of the heart failure (see section 5.1).

Use in patients with impaired hepatic function:

The half life of amlodipine is prolonged in patients with impaired liver function; dosage recommendations have not been established. Amlodipine should therefore be administered with caution in these patients.

Use in elderly patients

In elderly patients, caution is advised when the dosage is increased (see section 5.2).

Use in renal failure

Amlodipine may be used in such patients at normal doses. Changes in amlodipine plasma concentrations are not correlated with degree of renal impairment. Amlodipine is not dialyzable

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Effects of other medicinal products on amlodipine

CYP3A4 inhibitors: With concomitant use with the CYP3A4 inhibitor erythromycin in young patients and diltiazem in elderly patients respectively the plasma concentration of amlodipine increased by 22% and 50 % respectively. However, the clinical relevance of this finding is uncertain. It cannot be ruled out that strong inhibitors of CYP3A4 (e.g. ketoconazole, itraconazole, ritonavir) may increase the plasma concentrations of amlodipine to a greater extent than diltiazem. Amlodipine should be used with caution together with CYP3A4 inhibitors. However, no adverse events attributable to such interaction have been reported.

CYP3A4 inducers: There is no data available regarding the effect of CYP3A4 inducers on amlodipine. The concomitant use of CYP3A4 inducers (e.g. rifampicin, hypericum perforatum) may give a lower plasma concentration of amlodipine. Amlodipine should be used with caution together with CYP3A4 inducers.

In clinical interaction studies grapefruit juice, cimetidine, aluminium/ magnesium (antacid) and sildenafil did not affect the pharmacokinetics of amlodipine.

Effects of amlodipine on other medicinal products

The blood pressure lowering effects of amlodipine adds to the blood pressure-lowering effects of other antihypertensive agents.

In clinical interaction studies, amlodipine did not affect the pharmacokinetics of atorvastatin, digoxin, ethanol (alcohol), warfarin or cyclosporin.

There is no effect of amlodipine on laboratory parameters.

4.6 Pregnancy And Lactation

Pregnancy

The safety of amlodipine in human pregnancy has not been established.

Reproductive studies in rats have shown no toxicity except for delayed date of delivery and prolonged duration of labour at dosages 50 times greater than the maximum recommended dosage for humans.

Use in pregnancy is only recommended when there is no safer alternative and when the disease itself carries greater risk for the mother and foetus.

Lactation

It is not known whether amlodipine is excreted in breast milk. A decision on whether to continue/discontinue breast-feeding or to continue/discontinue therapy with amlodipine should be made taking into account the benefit of breast-feeding to the child and the benefit of amlodipine therapy to the mother.

4.7 Effects On Ability To Drive And Use Machines

Amlodipine can have minor or moderate influence on the ability to drive and use machines. If patients taking amlodipine suffer from dizziness, headache, fatigue or nausea the ability to react may be impaired.

4.8 Undesirable Effects

The following undesirable effects have been observed and reported during treatment with amlodipine with the following frequencies: Very common (

System Organ Class	Frequency	Undesirable effects
Blood and the lymphatic system disorders	Very Rare	Leukocytopenia, thrombocytopenia
Immune system disorders	Very Rare	Allergic reactions
Metabolism and nutrition disorders	Very Rare	Hyperglycaemia
Psychiatric disorders	Uncommon	Insomnia, mood changes (including anxiety), depression
Rare	Confusion
Nervous system disorders	Common	Somnolence, dizziness, headache (especially at the beginning of the treatment)
Uncommon	Tremor, dysgeusia, syncope, hypoesthesia, paresthesia
Very Rare	Hypertonia, peripheral neuropathy
Eye disorders	Uncommon	Visual disturbance (including diplopia)
Ear and labyrinth disorders	Uncommon	Tinnitus
Cardiac disorders	Uncommon	Palpitations
Very Rare	Myocardial infarction, arrhythmia (including bradycardia, ventricular tachycardia and atrial fibrillation)
Vascular disorders	Common	Flushing
Uncommon	Hypotension
Very Rare	Vasculitis
Respiratory, thoracic and medicinal disorders	Uncommon	Dyspnoea, rhinitis
Very Rare	Cough
Gastrointestinal disorders	Common	Abdominal pain, nausea
Uncommon	Vomiting, dyspepsia, altered bowel habits (including diarrohea and constipation), dry mouth
Very Rare	Pancreatitis, gastritis, gingival hyperplasia
Hepato-biliary disorders	Very Rare	Hepatitis, jaundice, hepatic enzymes increased*
Skin and subcutaneous tissue disorders	Uncommon	Alopecia, purpura, skin discolouration, hyperhydrosis, pruritus, rash, exanthema
Very Rare	Angioedema, erythema multiforme, urticaria, exfoliative dermatitis, Stevens-Johnson syndrome, Quincke oedema, photosensitivity
Musculoskeletal, connective tissue and bone disorders	Common	Ankle swelling
Uncommon	Arthralgia, myalgia, muscle cramps, back pain
Renal and urinary disorders	Uncommon	Micturition disorder, nocturia, increased urinary frequency
Reproductive system and breast disorders	Uncommon	Impotence, gynecomastia
General disorders and administration site conditions	Common	Oedema, fatigue
Uncommon	Chest pain, asthenia, pain, malaise
Investigations	Uncommon	Weight increase, weight decrease

*mostly consistent with cholestatis

4.9 Overdose

In humans experience with intentional overdose is limited

Symptoms:

Available data suggest that gross overdosage could result in excessive peripheral vasodilatation and possibly reflex tachycardia. Marked and probably prolonged systemic hypotension up to and including shock with fatal outcome have been reported.

Treatment:

Clinically significant hypotension due to amlodipine overdosage calls for active cardiovascular support including frequent monitoring of cardiac and respiratory function, elevation of extremities and attention to circulating fluid volume and urine output.

A vasoconstrictor may be helpful in restoring vascular tone and blood pressure, provided that there is no contraindication to its use. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade.

Gastric lavage may be worthwhile in some cases. In healthy volunteers the use of charcoal up to 2 hours after administration of amlodipine 10 mg has been shown to reduce the absorption rate of amlodipine.

Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Pharmacotherapeutic group: Selective calcium channel blockers with mainly vascular effects; Dihydropyridine derivatives

ATC code: C 08 CA 01

Amlodipine is a calcium antagonist that inhibits the influx of calcium ions into the cardiac and vascular smooth muscle. The mechanism of the antihypertensive action is the result of the direct relaxing effect on the arterial smooth muscle.

The mechanism that enables amlodipine to reduce angina pectoris has not been completely clarified; however, the two following mechanisms are involved:

1. Amlodipine dilates peripheral arterioles and thus, reduces the total peripheral resistance (afterload) against which the heart works. This reduction of the heart load leads to a reduction of the energy consumption as well as of the oxygen requirements of the myocardium.

2. The dilatation of the main coronary vessels and coronary arterioles probably is involved in the mechanism of action of amlodipine. This dilatation increases the myocardial oxygen supply in patients suffering from Prinzmetal's angina pectoris.

In patients suffering from hypertension, once daily administration produces a clinically significant reduction in blood pressure (both in lying and standing position), lasting for 24 hours.

In patients suffering from angina pectoris, once daily administration increases total exercise time, the time to occurrence of angina and the time to a 1 mm ST segment depression. Amlodipine reduces both the frequency of anginal attacks and the use of glyceryl trinitrate tablets.

Use in Patients with Heart Failure

Haemodynamic studies and exercise based controlled clinical trials in NYHA Class II-IV heart failure patients have shown that amlodipine did not lead to clinical deterioration as measured by exercise tolerance, left ventricular ejection fraction and clinical symptomatology.

A placebo controlled study (PRAISE) designed to evaluate patients in NYHA Class III-IV heart failure receiving digoxin, diuretics and angiotensin-converting enzyme (ACE) inhibitors has shown that amlodipine did not lead to an increase in risk of mortality or combined mortality and morbidity in patients with heart failure.

In a follow-up, long-term, placebo controlled study (PRAISE-2) of amlodipine in patients with NYHA III and IV heart failure without clinical symptoms or objective findings suggestive of underlying ischaemic disease, on stable doses of ACE inhibitors, digitalis, and diuretics, amlodipine had no effect on total or cardiovascular mortality. In this same population amlodipine was associated with increased reports of pulmonary oedema despite no significant difference in the incidence of worsening heart failure as compared to placebo.

Use in Children with Hypertension, aged 6-17 years

In a study involving 268 children aged 6-17 years with predominantly secondary hypertension, comparison of a 2.5mg dose, and 5.0mg dose of amlodipine with placebo, showed that both doses reduced Systolic Blood Pressure significantly more than placebo. The difference between the two doses was not statistically significant.

The long-term effects of amlodipine on growth, puberty and general development have not been studied. The long-term efficacy of amlodipine on therapy in childhood to reduce cardiovascular morbidity and mortality in adulthood have also not been established.

5.2 Pharmacokinetic Properties

Absorption and distribution

After oral administration of therapeutic doses, amlodipine is slowly absorbed from the gastrointestinal tract. The bioavailability of amlodipine is not influenced by concomitant intake of food. The absolute bioavailability of the unchanged active substance is approximately 64-80%. Peak plasma concentrations are reached within 6-12 hours after administration. The volume of distribution is approximately 20 l/kg. The pKa of amlodipine is 8.6. In vitro plasma protein binding is approximately 98%.

Metabolism and elimination

The plasma half-life varies between 35 and 50 hours. Steady-state plasma concentration is reached after 7-8 days.

Amlodipine is extensively metabolised into inactive metabolites. Approximately 60% of the administered dose is excreted in the urine, 10% of which is in a non-metabolised form.

Use in Elderly

The time to reach peak plasma concentrations of amlodipine is similar in elderly and younger subjects. Amlodipine clearance tends to be decreased with resulting increases in AUC and elimination half life in elderly patients. Increases in AUC and elimination half life in patients with congestive heart failure were as expected for the patient agze group study (See Section 4.4).

Patients with impaired renal function

Amlodipine is extensively metabolised into inactive metabolites. 10% of the parent compound is excreted unchanged in the urine. The changes in the plasma concentration of amlodipine are not related to the degree of renal impairment. These patients can be treated with a normal dosage of amlodipine. Amlodipine is not dialyzable.

Patients with impaired hepatic function

The half-life of amlodipine is prolonged in patients with impaired hepatic function.

Use in Children and Adolescents

A population PK study has been conducted in 74 hypertensive children aged from 12 months to 17 years (with 34 patients aged 6 to 12 years and 28 patients aged 13 to 17 years) receiving amlodipine between 1.25 and 20 mg given either once or twice daily. In children 6 to 12 years and in adolescents 13-17 years of age the typical oral clearance (CL/F) was 22.5 and 27.4 L/hr respectively in males and 16.4 and 21.3 L/hr respectively in females. Large variability in exposure between individuals was observed. Data reported in children below 6 years is limited.

5.3 Preclinical Safety Data

Animal studies have shown no special risks for humans. This is based on information from pharmacological studies concerning safety and on information on repeat dose toxicity, genotoxicity and carcinogenicity. Reproductive studies in animals have shown a delayed parturition, difficult labour and an increased foetal and neonatal death at high dosages.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Microcrystalline cellulose

Calcium hydrogen phosphate, anhydrous

Sodium starch glycolate

Magnesium stearate

6.2 Incompatibilities

Not applicable.

6.3 Shelf Life

3 years

6.4 Special Precautions For Storage

This medicinal product does not require any special storage conditions.

6.5 Nature And Contents Of Container

PVC/ PVdC-Aluminium blister.

7, 10, 14, 15, 20, 28, 30, 50, 56, 60, 84, 90, 98, 100, 120, 200, 250, 300 and 500 tablets

Not all pack sizes may be marketed.

6.6 Special Precautions For Disposal And Other Handling

No special requirements.

7. Marketing Authorisation Holder

Milpharm Limited

Ares, Odyssey Business Park

West End Road

South Ruislip HA4 6QD

United Kingdom

8. Marketing Authorisation Number(S)

PL 16363/0249

9. Date Of First Authorisation/Renewal Of The Authorisation

11/05/2011

10. Date Of Revision Of The Text

11/05/2011

insulin aspart and insulin aspart protamine

Generic Name: insulin aspart and insulin aspart protamine (IN su lin AS part, IN su lin AS part PRO ta meen)

Brand Names: NovoLOG Mix 70/30, NovoLOG Mix 70/30 FlexPen, NovoLOG Mix 70/30 PenFill

What is insulin aspart and insulin aspart protamine?

Insulin is a hormone that is produced in the body. It works by lowering levels of glucose (sugar) in the blood. Insulin aspart and insulin aspart protamine is a faster-acting form of insulin than regular human insulin.

Insulin aspart and insulin aspart protamine is used to treat type 1 (insulin-dependent) diabetes in adults.

Insulin aspart and insulin aspart protamine may also be used for purposes not listed in this medication guide.

What is the most important information I should know about insulin aspart and insulin aspart protamine?

Take care not to let your blood sugar get too low. Low blood sugar (hypoglycemia) can occur if you skip a meal, exercise too long, drink alcohol, or are under stress. Symptoms include headache, hunger, weakness, sweating, tremors, irritability, or trouble concentrating. Carry hard candy or glucose tablets with you in case you have low blood sugar. Other sugar sources include orange juice and milk. Be sure your family and close friends know how to help you in an emergency.

Also watch for signs of blood sugar that is too high (hyperglycemia). These symptoms include increased thirst, increased urination, loss of appetite, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, and weight loss. Your blood sugar will need to be checked often, and you may need to adjust your insulin aspart and insulin aspart protamine dose.

Never share an injection pen or cartridge with another person. Sharing injection pens or cartridges can allow disease such as hepatitis or HIV to pass from one person to another.

What should I discuss with my healthcare provider before using insulin aspart and insulin aspart protamine?

Do not use this medication if you are allergic to insulin, or if you are having an episode of hypoglycemia (low blood sugar).

To make sure you can safely use insulin aspart and insulin aspart protamine, tell your doctor if you have liver or kidney disease.

This medication is only part of a complete program of treatment that may also include diet, exercise, weight control, foot care, eye care, dental care, and testing your blood sugar. Follow your diet, medication, and exercise routines very closely. Changing any of these factors can affect your blood sugar levels.

FDA pregnancy category B. Insulin aspart and insulin aspart protamine is not expected to harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether insulin aspart and insulin aspart protamine passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I use insulin aspart and insulin aspart protamine?

Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Insulin aspart and insulin aspart protamine is injected under the skin. You will be shown how to use injections at home. Do not self-inject this medicine if you do not fully understand how to give the injection and properly dispose of used needles and syringes.

Insulin aspart and insulin aspart protamine must not be given with an insulin pump, or mixed with other insulins. After using insulin aspart and insulin aspart protamine, you should eat a meal within 15 minutes. This medication is usually given with 2 meals per day.

Just before using this medication, roll the vial (medicine bottle) 10 times between the palms of your hands, until the medicine looks white and cloudy. Then give the injection right away.

If you use the injection pen, turn it upside down so the glass ball inside it moves from one end to the other. Do this at least 10 times, until the medicine looks white and cloudy, then give the injection right away. Repeat this procedure each time you use the injection pen.

Choose a different place in your injection skin area each time you use this medication. Do not inject into the same place two times in a row.

Throw away used needles in a puncture-proof container (ask your pharmacist where you can get one and how to dispose of it). Keep this container out of the reach of children and pets.

Never share an injection pen or cartridge with another person. Sharing injection pens or cartridges can allow disease such as hepatitis or HIV to pass from one person to another. Know the signs of low blood sugar (hypoglycemia) and how to recognize them: headache, hunger, weakness, sweating, tremors, irritability, or trouble concentrating.

Always keep a source of sugar available in case you have symptoms of low blood sugar. Sugar sources include orange juice, glucose gel, candy, or milk. If you have severe hypoglycemia and cannot eat or drink, use an injection of glucagon. Your doctor can give you a prescription for a glucagon emergency injection kit and tell you how to give the injection.

Also watch for signs of blood sugar that is too high (hyperglycemia). These symptoms include increased thirst, increased urination, loss of appetite, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, and weight loss.

Check your blood sugar carefully during a time of stress or illness, if you travel, exercise more than usual, drink alcohol, or skip meals. These things can affect your glucose levels and your dose needs may also change.

Your doctor may want you to stop taking insulin aspart and insulin aspart protamine for a short time if you become ill, have a fever or infection, or if you have surgery or a medical emergency.

Ask your doctor how to adjust your insulin aspart and insulin aspart protamine dose if needed. Do not change your medication dose or schedule without your doctor's advice. Storing unopened vials or injection pens: Keep in the carton and store in a refrigerator, protected from light. Throw away any insulin not used before the expiration date on the medicine label. Unopened vials or injection pens may also be stored at room temperature for up to 28 days, away from heat and bright light. Throw away any insulin not used within 28 days. Storing vials after your first use: You may keep "in-use" vials in the refrigerator, protected from light. Use within 28 days. You may also keep in-use" vials at room temperature. Use within 28 days. Protect from light. Storing injection pens after your first use: Keep the "in-use" injection pen at room temperature and use within 28 days. Do not refrigerate. Protect from light.

Do not freeze this medication, and throw away the medication if it has become frozen.

What happens if I miss a dose?

Since insulin aspart and insulin aspart protamine is used before meals, you may not be on a timed dosing schedule. Whenever you use this medication, be sure to eat a meal within 15 minutes. Do not use extra insulin aspart and insulin aspart protamine to make up a missed dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.Overdose can cause life-threatening hypoglycemia.

Symptoms of severe hypoglycemia include extreme weakness, blurred vision, sweating, trouble speaking, tremors, stomach pain, confusion, and seizure (convulsions).

What should I avoid while using insulin aspart and insulin aspart protamine?

Avoid drinking alcohol. It lowers blood sugar and may interfere with your diabetes treatment.

Insulin aspart and insulin aspart protamine side effects

Get emergency medical help if you have any of these signs of insulin allergy: itching skin rash over the entire body, wheezing, trouble breathing, fast heart rate, sweating, or feeling like you might pass out.

Hypoglycemia, or low blood sugar, is the most common side effect of insulin. Symptoms include headache, hunger, weakness, sweating, tremors, irritability, trouble concentrating, rapid breathing, fast heartbeat, fainting, or seizure (severe hypoglycemia can be fatal). Carry hard candy or glucose tablets with you in case you have low blood sugar.

Call your doctor at once if you have a serious side effect such as:

• 
  

  vision changes;

  
  


• 
  

  swelling in your hands or feet; or

  
  


• 
  

  low potassium (confusion, uneven heart rate, extreme thirst, increased urination, leg discomfort, muscle weakness or limp feeling).

  
  

Tell your doctor if you have itching, swelling, redness, or thickening of the skin where you inject insulin aspart and insulin aspart protamine.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Insulin aspart and insulin aspart protamine Dosing Information

Usual Adult Dose for Diabetes Mellitus Type I:

Insulin aspart is a short acting insulin with a rapid onset and should be given immediately before meals. 50 to 70% of the daily insulin requirement may be provided by aspart and the remainder by an intermediate or long-acting insulin.

Insulin dosage should be individualized to achieve/maintain a target blood glucose level and is determined by various factors including body weight, body fat, physical activity, insulin sensitivity, blood glucose levels, and target blood glucose.

Conventional regimen: The total daily insulin dose is administered as a mixture of rapid/short-acting and intermediate-acting insulins in 1 to 2 injections. Twice daily injections are preferred for better glycemic control. With the 2-injection regimen, generally two-thirds of the daily dose is given before breakfast and one-third is given before the evening meal.

Intensive regimen: The total daily dose is administered as 3 or more injections or by continuous subcutaneous infusion to cover basal and pre-meal bolus insulin requirements. The basal requirement is approximately 30 to 50% of the total dose, given as intermediate or long-acting insulin (NPH, zinc, extended zinc, lispro-protamine, glargine), 1 to 2 times daily. Meal boluses are approximately 50 to 70% of the total dose, given as rapid/short-acting insulin (regular, aspart, lispro) 2 to 5 times daily before meals. Common regimens include injections of rapid/short acting insulin before each meal along with injections of intermediate or long-acting insulin in the morning and/or evening. Dosage adjustments are made to achieve target blood glucose levels and are based on frequent blood glucose measurements, diet and exercise levels.

Total daily insulin requirements:
Initial dose: 0.5 to 0.8 unit/kg/day subcutaneously
Honeymoon phase: 0.2 to 0.5 unit/kg/day subcutaneously
Split dose therapy: 0.5 to 1.2 unit/kg/day subcutaneously
Insulin resistance: 0.7 to 2.5 units/kg/day subcutaneously

Usual Adult Dose for Diabetes Mellitus Type II:

Insulin aspart is a short acting insulin with a rapid onset and should be given immediately before meals. 50 to 70% of the daily insulin requirement may be provided by aspart and the remainder by an intermediate or long-acting insulin.

Diet and lifestyle modifications are recommended as initial treatment for type II diabetes, followed by oral agents. Insulin may be considered if patients are very hyperglycemic or symptomatic and/or not controlled with oral agents. Insulin may exacerbate obesity, further increase insulin resistance, and increase the frequency of hypoglycemia.

Insulin dosage should be individualized to achieve/maintain a target blood glucose level and is determined by various factors including body weight, body fat, physical activity, insulin sensitivity, blood glucose levels, and target blood glucose.

Conventional regimen:
Initial dose, monotherapy: Total insulin requirement: 0.1 unit/kg/day. When insulin is used alone, twice daily injections are recommended for better glycemic control. The total daily insulin dose is administered as a mixture of rapid/short-acting and intermediate-acting insulins in 1 to 2 injections. With the 2-injection regimen, generally two-thirds of the daily dose is given before breakfast and one-third is given before the evening meal. Once daily injections are sometimes used in children with suboptimal compliance; however, this may lead to more nocturia, fasting hyperglycemia, morning glucosuria, and a risk of ketoacidosis if the doses are missed.
Maintenance dose, monotherapy: Total daily insulin requirements may progress to 1.5 to 2.5 units/kg or higher in patients with obesity and insulin resistance.

Intensive regimen:
The necessity for and efficacy of intensive insulin therapy in type II diabetes has been controversial. The total daily dose is administered as 3 or more injections or by continuous subcutaneous infusion to cover basal and pre-meal bolus insulin requirements. This method may be appropriate for closely supervised and highly motivated older children or adolescents who are able to inject their insulin, monitor their blood glucose, and recognize hypoglycemia. The basal requirement is approximately 30 to 50% of the total dose, given as intermediate or long-acting insulin (NPH,zinc, extended zinc, lispro-protamine, glargine), 1 to 2 times daily. Meal boluses are approximately 50 to 70% of the total dose, given as rapid/short-acting insulin (regular, aspart, lispro) 2 to 5 times daily before meals. Common regimens include injections of rapid/short acting insulin before each meal along with injections of intermediate or long-acting insulin in the morning and/or evening. Dosage adjustments are made to achieve target blood glucose levels and are based on frequent blood glucose measurements, diet and exercise levels.
Initial dose, monotherapy: 0.5 to 1.5 unit/kg/day subcutaneously.
Maintenance dose, monotherapy: Total daily insulin requirements may progress to 2.5 units/kg or higher in patients with obesity and insulin resistance.

What other drugs will affect insulin aspart and insulin aspart protamine?

Tell your doctor about all other medications you use, especially:

• 
  

  albuterol (Proventil, Ventolin);

  
  


• 
  

  clonidine (Catapres);

  
  


• 
  

  disopyramide (Norpace);

  
  


• 
  

  niacin (Advicor, Niaspan, Niacor, Simcor, Slo-Niacin, and otheres);

  
  


• 
  

  pramlintide (Symlin);

  
  


• 
  

  fenofibrate (Antara, Lipofen, Triglide), fenofibric acid (Trilipix), or gemfibrozil (Lopid);

  
  


• 
  

  enalapril (Vasotec), lisinopril (Prinivil, Zestril), ramipril (Altace), and others;

  
  


• 
  

  aspirin or other salicylates (including Pepto-Bismol);

  
  


• 
  

  birth control pills and other hormones;

  
  


• 
  

  diet pills or medicines to treat asthma, colds or allergies;

  
  


• 
  

  diuretics (water pills);

  
  


• 
  

  a monoamine oxidase inhibitor (MAOI);

  
  


• 
  

  phenothiazines (Phenergan and others);

  
  


• 
  

  thyroid medicine (Synthroid and others);

  
  


• 
  

  a beta-blocker (Tenormin, Normodyne, Toprol, Coreg, Inderal, and others);

  
  


• 
  

  medicines to treat psychiatric disorders (Abilify, Clozaril, Zyprexa, Compazine, Risperdal, and others);

  
  


• 
  

  steroids (prednisone and others); or

  
  


• 
  

  sulfa drugs (Bactrim, Septra, and others).

  
  

This list is not complete and there are many other medicines that can increase or decrease the effects of insulin on lowering your blood sugar. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

More insulin aspart and insulin aspart protamine resources

• Insulin aspart and insulin aspart protamine Use in Pregnancy & Breastfeeding
• Insulin aspart and insulin aspart protamine Drug Interactions
• Insulin aspart and insulin aspart protamine Support Group
• 2 Reviews for Insulin aspart and insulin aspart protamine - Add your own review/rating

Compare insulin aspart and insulin aspart protamine with other medications

• Diabetes, Type 1
• Diabetes, Type 2

Where can I get more information?

• Your pharmacist can provide more information about insulin aspart and insulin aspart protamine.

Afinitor

Pronunciation: E-ver-OH-li-mus
Generic Name: Everolimus
Brand Name: Afinitor

Afinitor is used for:

Treating advanced kidney cancer in certain patients. It is used to treat a certain type of pancreatic cancer. It is also used to treat a type of brain tumor (subependymal giant cell astrocytoma [SEGA]) in certain patients. It may also be used for other conditions as determined by your doctor.

Afinitor is a kinase inhibitor. It works by preventing the growth of cancer cells.

Do NOT use Afinitor if:

• you are allergic to any ingredient in Afinitor or to other similar medicines (eg, sirolimus, temsirolimus)


• you have severe liver problems


• you are taking atazanavir, clarithromycin, indinavir, itraconazole, ketoconazole, nefazodone, nelfinavir, ritonavir, saquinavir, St. John's wort, telithromycin, or voriconazole

Contact your doctor or health care provider right away if any of these apply to you.

Before using Afinitor:

Some medical conditions may interact with Afinitor. Tell your doctor or pharmacist if you have any medical conditions, especially if any of the following apply to you:

• if you are pregnant, planning to become pregnant, or are breast-feeding


• if you are able to become pregnant


• if you are taking any prescription or nonprescription medicine, herbal preparation, or dietary supplement


• if you have allergies to medicines, foods, or other substances


• if you have diabetes or high blood sugar, high cholesterol, bone marrow problems, certain blood problems (eg, low white blood cell or platelet levels), a weakened immune system, or a history of lung or breathing problems


• if you have any type of infection (including fungal infections) or a history of persistent or recurring infection


• if you have or have a history of hepatitis B or other liver problems, or kidney problems


• if you have recently received or will be receiving a vaccine (eg, measles, mumps), or if you will be in close contact with anyone who has received a live vaccine


• if you take medicine that may weaken your immune system. Check with your doctor or pharmacist if you are unsure if any of your medicines may weaken your immune system

Some MEDICINES MAY INTERACT with Afinitor. Tell your health care provider if you are taking any other medicines, especially any of the following:

• Angiotensin-converting enzyme (ACE) inhibitors (eg, lisinopril) because they may increase the risk of a serious side effect called angioedema (swelling of the hands, face, lips, eyes, throat, or tongue; difficulty swallowing or breathing; unusual hoarseness)


• Anticoagulants (eg, warfarin) because the risk of severe bleeding may be increased


• Aprepitant, azole antifungals (eg, fluconazole, itraconazole, ketoconazole, voriconazole), calcium channel blockers (eg, diltiazem, verapamil), cyclosporine, delavirdine, HIV protease inhibitors (eg, ritonavir), macrolide antibiotics (eg, clarithromycin, erythromycin), nefazodone, or telithromycin because they may increase the risk of Afinitor's side effects


• Barbiturates (eg, phenobarbital), carbamazepine, dexamethasone, hydantoins (eg, phenytoin), rifamycins (eg, rifabutin, rifampin, rifapentine), or St. John's wort because they may decrease Afinitor's effectiveness

This may not be a complete list of all interactions that may occur. Ask your health care provider if Afinitor may interact with other medicines that you take. Check with your health care provider before you start, stop, or change the dose of any medicine.

How to use Afinitor:

Use Afinitor as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• An extra patient leaflet is available with Afinitor. Talk to your pharmacist if you have questions about this information.


• Take Afinitor by mouth with or without food. It is important to take it consistently with regard to meals. If you take it with food, try to always take it with food. If you prefer to take it on an empty stomach, then always try to take it on an empty stomach.


• Swallow Afinitor whole. Do not break, crush, or chew before swallowing. Do not take a tablet that has been broken or crushed.


• Take Afinitor with a full glass of water (8 oz/240 mL).


• Do not remove the tablet from the blister package until you are ready to take Afinitor.


• If you cannot swallow Afinitor, you may dissolve the tablet in a glass containing 2 tablespoons (30 mL) of water. Stir to mix completely, and drink immediately. Do not store the mixture for use at a later time. After you drink the mixture, rinse the glass with another 2 tablespoons (30 mL) of water and drink to be sure that you receive the entire dose of Afinitor.


• Do not eat grapefruit or drink grapefruit juice while you use Afinitor.


• Afinitor works best if it is taken at the same time each day.


• If you miss a dose of Afinitor, take it as soon as possible. If it is more than 6 hours after you normally take your dose, skip the missed dose and go back to your regular dosing schedule the next day. Do not take 2 doses at once.

Ask your health care provider any questions you may have about how to use Afinitor.

Important safety information:

• Afinitor may cause dizziness. This effect may be worse if you take it with alcohol or certain medicines. Take Afinitor with caution. Do not drive or perform other possibly unsafe tasks until you know how you react to it.


• Afinitor may cause dizziness; alcohol, hot weather, exercise, or fever may increase these effects. To prevent this, sit up or stand slowly, especially in the morning. Sit or lie down at the first sign of dizziness.


• Tell your doctor or dentist that you take Afinitor before you receive any medical or dental care, emergency care, or surgery.


• Contact your doctor if you have a wound that does not heal properly while you are using Afinitor.


• Serious and sometimes fatal kidney problems have occurred in patients who have taken Afinitor. Contact your doctor immediately if you experience decreased urination or if you have any questions or concerns about this information.


• Pain, discomfort, or sores of the mouth or tongue may occur while you are taking Afinitor. Check with your doctor about how to treat these effects. Do not treat these effects with mouthwashes that contain alcohol or peroxide unless your doctor tells you otherwise.


• Afinitor may lower the ability of your body to fight infection. Avoid contact with people who have colds or infections. Tell your doctor if you notice signs of infection like fever, sore throat, rash, or chills.


• Do not receive a live vaccine (eg, measles, mumps) while you are taking Afinitor. Avoid close contact with anyone who has recently received a live vaccine. Talk with your doctor before you receive any vaccine.


• Afinitor may raise your blood sugar. High blood sugar may make you feel confused, drowsy, or thirsty. It can also make you flush, breathe faster, or have a fruit-like breath odor. If these symptoms occur, tell your doctor right away.


• Noninfectious pneumonitis is a severe and possibly fatal reaction that may occur with the use of Afinitor. Tell your doctor right away if you develop fever, shortness of breath, cough, or any other new or worsening breathing problems.


• If you may become pregnant, you must use an effective form of birth control while you take Afinitor and for 8 weeks after you stop taking it. If you have questions about effective birth control, talk with your doctor.


• Lab tests, including kidney function, everolimus levels, blood cholesterol levels, blood glucose levels, and complete blood cell counts, may be performed while you use Afinitor. These tests may be used to monitor your condition or check for side effects. Be sure to keep all doctor and lab appointments.


• Afinitor should be used with extreme caution in CHILDREN younger than 3 years who have SEGA; safety and effectiveness in these children have not been confirmed.


• PREGNANCY and BREAST-FEEDING: Afinitor may cause harm to the fetus. Do not become pregnant while you are taking it and for 8 weeks after you stop Afinitor. If you think you may be pregnant, contact your doctor. You will need to discuss the benefits and risks of taking Afinitor while you are pregnant. It is not known if Afinitor is found in breast milk. Do not breast-feed while taking Afinitor.

Possible side effects of Afinitor:

All medicines may cause side effects, but many people have no, or minor, side effects. Check with your doctor if any of these most COMMON side effects persist or become bothersome:

Acne; constipation; diarrhea; dizziness; dry skin; fingernail or toenail changes; headache; joint, back, arm, or leg pain; loss of appetite; mild itching; muscle spasms; nausea; nosebleed; stomach pain or upset; stuffy or runny nose; taste changes; tiredness or weakness; trouble sleeping; vomiting; weight loss.

Seek medical attention right away if any of these SEVERE side effects occur:

Severe allergic reactions (rash; hives; itching; difficulty breathing or swallowing; flushing; tightness in the chest; swelling of the mouth, face, lips, or tongue; unusual hoarseness); bloody stools; burning, numbness, or tingling (especially of the palms of the hands and soles of the feet); chest pain; decreased, difficult, or painful urination; dry mouth or increased thirst; fast or irregular heartbeat; fever, chills, or persistent sore throat; interrupted breathing while sleeping; new or worsening cough; pain, discomfort, or sores of the mouth or tongue; personality changes; seizure; severe or persistent diarrhea, nausea, stomach pain, or vomiting; severe or persistent dizziness or headache; severe or persistent tiredness or weakness; shortness of breath or other breathing problems; swelling of the arms, hands, feet, or ankles; symptoms of high blood sugar (eg, increased hunger, thirst, or urination; confusion; unusual drowsiness); unusual bruising or bleeding; wheezing; yellowing of the eyes or skin.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider. Call your doctor for medical advice about side effects. To report side effects to the appropriate agency, please read the Guide to Reporting Problems to FDA.

See also: Afinitor side effects (in more detail)

If OVERDOSE is suspected:

Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local poison control center, or emergency room immediately.

Proper storage of Afinitor:

Store Afinitor at 77 degrees F (25 degrees C). Brief storage at temperatures between 59 and 86 degrees F (15 and 30 degrees C) is permitted. Store in original package away from heat, moisture, and light. Do not store in the bathroom. Keep Afinitor out of the reach of children and away from pets.

General information:

• If you have any questions about Afinitor, please talk with your doctor, pharmacist, or other health care provider.


• Afinitor is to be used only by the patient for whom it is prescribed. Do not share it with other people.


• If your symptoms do not improve or if they become worse, check with your doctor.


• Check with your pharmacist about how to dispose of unused medicine.

This information is a summary only. It does not contain all information about Afinitor. If you have questions about the medicine you are taking or would like more information, check with your doctor, pharmacist, or other health care provider.

Issue Date: February 1, 2012

Database Edition 12.1.1.002

Copyright © 2012 Wolters Kluwer Health, Inc.

More Afinitor resources

• Afinitor Side Effects (in more detail)
• Afinitor Dosage
• Afinitor Use in Pregnancy & Breastfeeding
• Drug Images
• Afinitor Drug Interactions
• Afinitor Support Group
• 1 Review for Afinitor - Add your own review/rating

• Afinitor Prescribing Information (FDA)


• Afinitor Consumer Overview


• Afinitor Monograph (AHFS DI)


• Afinitor Advanced Consumer (Micromedex) - Includes Dosage Information


• Everolimus Professional Patient Advice (Wolters Kluwer)


• Zortress Prescribing Information (FDA)


• Zortress Consumer Overview

Compare Afinitor with other medications

• Brain Tumor
• Pancreatic Cancer
• Renal Cell Carcinoma

Tykerb

Generic Name: lapatinib (Oral route)

la-PA-ti-nib

Oral route(Tablet)

Hepatotoxicity has been observed in clinical trials and postmarketing experience. The hepatotoxicity may be severe and deaths have been reported. Causality of the deaths is uncertain .

Commonly used brand name(s)

In the U.S.

• Tykerb

Available Dosage Forms:

• Tablet

Therapeutic Class: Antineoplastic Agent

Pharmacologic Class: Tyrosine Kinase Inhibitor

Uses For Tykerb

Lapatinib belongs to the group of medicines called antineoplastics or cancer medicines. It is used in combination with capecitabine to treat advanced or metastatic HER2-receptor positive breast cancer (breast cancer that has already spread) after other treatments have failed.

Lapatinib is also used together with letrozole to treat postmenopausal women (women who no longer make estrogen) with hormone-receptor positive and HER2-receptor positive metastatic breast cancer.

Lapatinib interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal cells may also be affected by the medicine, other effects will also occur. Some of these may be serious and must be reported to your doctor. Other effects may not be serious but may cause concern.

Before you begin treatment with lapatinib, you and your doctor should talk about the good this medicine will do as well as the risks of using it.

This medicine is available only with your doctor's prescription.

Before Using Tykerb

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies have not been performed on the relationship of age to the effects of lapatinib in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of lapatinib in the elderly.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	D	Studies in pregnant women have demonstrated a risk to the fetus. However, the benefits of therapy in a life threatening situation or a serious disease, may outweigh the potential risk.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Cisapride


• Dronedarone


• Fluconazole


• Mesoridazine


• Pimozide


• Posaconazole


• Saquinavir


• Sparfloxacin


• Thioridazine

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Alfuzosin


• Amiodarone


• Amitriptyline


• Amoxapine


• Apomorphine


• Arsenic Trioxide


• Asenapine


• Astemizole


• Atazanavir


• Azithromycin


• Carbamazepine


• Chloroquine


• Chlorpromazine


• Ciprofloxacin


• Citalopram


• Clarithromycin


• Clomipramine


• Clozapine


• Crizotinib


• Dasatinib


• Desipramine


• Dexamethasone


• Digoxin


• Disopyramide


• Dofetilide


• Dolasetron


• Droperidol


• Erythromycin


• Flecainide


• Gatifloxacin


• Gemifloxacin


• Granisetron


• Halofantrine


• Haloperidol


• Ibutilide


• Iloperidone


• Imipramine


• Indinavir


• Itraconazole


• Ketoconazole


• Levofloxacin


• Lopinavir


• Lumefantrine


• Mefloquine


• Methadone


• Moxifloxacin


• Nefazodone


• Nelfinavir


• Nilotinib


• Norfloxacin


• Nortriptyline


• Octreotide


• Ofloxacin


• Ondansetron


• Paliperidone


• Pazopanib


• Perflutren Lipid Microsphere


• Phenobarbital


• Phenytoin


• Procainamide


• Prochlorperazine


• Promethazine


• Propafenone


• Protriptyline


• Quetiapine


• Quinidine


• Quinine


• Ranolazine


• Rifabutin


• Rifampin


• Rifapentine


• Ritonavir


• Salmeterol


• Sodium Phosphate


• Sodium Phosphate, Dibasic


• Sodium Phosphate, Monobasic


• Solifenacin


• Sorafenib


• Sotalol


• St John's Wort


• Sunitinib


• Telavancin


• Telithromycin


• Terfenadine


• Tetrabenazine


• Toremifene


• Trazodone


• Trifluoperazine


• Trimipramine


• Vandetanib


• Vardenafil


• Vemurafenib


• Voriconazole


• Ziprasidone

Using this medicine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Paclitaxel

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

• Grapefruit Juice

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Diarrhea or


• Liver disease, history of or


• Lung disease (e.g., interstitial lung disease, pneumonitis), history of—Use with caution. May make these conditions worse.

• Heart disease, history of or


• Heart rhythm problems (e.g., congenital long QT syndrome) or


• Hypokalemia (low potassium in the blood) or


• Hypomagnesemia (low magnesium in the blood)—Use with caution. May cause side effects to become worse.

Proper Use of Tykerb

Medicines used to treat cancer are very strong and can have many side effects. Before receiving this medicine, make sure you understand all the risks and benefits. It is important for you to work closely with your doctor during your treatment.

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. Do not change your dose without checking first with your doctor.

This medicine comes with a patient information insert. Read and follow the instructions in the insert carefully. Ask your doctor if you have any questions.

This medicine should be taken at least one hour before or one hour after a meal. All of the lapatinib tablets are taken together as one dose each day.

Lapatinib is given together with capecitabine or letrozole. It is important that you take each medicine at the right time. Follow your doctor's instructions on when to take these medicines.

This medicine often causes diarrhea, nausea, and vomiting. However, it is very important that you continue to receive the medicine even if you begin to feel ill. Your doctor may give you medicines to help prevent these side effects.

Do not eat grapefruit or drink grapefruit juice while you are using this medicine.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For oral dosage form (tablets):
  
  • For advanced or metastatic breast cancer with capecitabine:
    
    • Adults—1250 milligrams (mg) or 5 tablets together as a single dose once a day for 21 days. Your doctor may tell you to repeat the 21-day cycle.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For metastatic breast cancer with letrozole:
    
    • Adults—1500 milligrams (mg) or 6 tablets together as a single dose once a day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using Tykerb

It is very important that your doctor check your progress at regular visits to make sure this medicine is working properly. Blood tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. If you think you have become pregnant while using the medicine, tell your doctor right away.

Serious heart problems can occur with this medicine. Check with your doctor right away if you are having fast, pounding, or irregular heartbeats; shortness of breath; or unusual tiredness or weakness.

Stop using this medicine and check with your doctor right away if you have pain or tenderness in the upper stomach; pale stools; dark urine; a loss of appetite; nausea; unusual tiredness or weakness; or yellow eyes or skin. These could be symptoms of a serious liver problem.

Check with your doctor immediately if severe diarrhea occurs while taking this medicine. You may need certain medicines to help manage or prevent the diarrhea.

Stop using this medicine and check with your doctor right away if you start having breathing problems, shortness of breath, a cough, chest pain, fever, or chills. These could be symptoms of a serious lung problem.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal (e.g., St. John's Wort) or vitamin supplements.

Tykerb Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

Less common

• Difficult or labored breathing


• fainting


• fast or irregular heartbeat


• severe diarrhea


• shortness of breath


• tightness in the chest


• unusual tiredness or weakness


• wheezing

Incidence not known

• Chest pain


• chills


• cough


• fever


• general feeling of discomfort or illness


• thickening of bronchial secretions


• troubled breathing

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Acid or sour stomach


• back pain


• belching


• cracked lips


• diarrhea


• difficulty with swallowing


• dry skin


• heartburn


• indigestion


• nausea


• pain in the arms or legs


• rash


• redness, swelling, or painful skin


• scaling of the skin on the hands and feet


• sleeplessness


• sores, ulcers, or white spots on the lips, tongue, or the inside of the mouth


• stomach discomfort, upset, or pain


• swelling or inflammation of the mouth


• tingling of the hands and feet


• trouble sleeping


• unable to sleep


• vomiting

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: Tykerb side effects (in more detail)

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More Tykerb resources

• Tykerb Side Effects (in more detail)
• Tykerb Dosage
• Tykerb Use in Pregnancy & Breastfeeding
• Tykerb Drug Interactions
• Tykerb Support Group
• 1 Review for Tykerb - Add your own review/rating

• Tykerb Prescribing Information (FDA)


• Tykerb Consumer Overview


• Tykerb Monograph (AHFS DI)


• Tykerb MedFacts Consumer Leaflet (Wolters Kluwer)


• Lapatinib Professional Patient Advice (Wolters Kluwer)

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