Stugeron Cinnarizine Tablets

Stugeron®

PRODUCT NAME

STUGERON® (cinnarizine)

DOSAGE FORMS AND STRENGTHS

Tablets

White, circular, biconvex, halfscored tablet with the inscription “JANSSEN” on one side and “S/25” on the other side. Each tablet contains 25 mg cinnarizine.

For excipients, see List of Excipients.

CLINICAL INFORMATION

Indications

Cerebral circulatory disorders

• Maintenance therapy for symptoms of cerebrovascular origin, including dizziness, ear buzzing (tinnitus), vascular headache, unsociability and irritability disorders, loss of memory and lack of concentration.

• Prophylaxis of migraine.

Disorders of balance

• Maintenance therapy for symptoms of labyrinthine disorders, including vertigo, dizziness, tinnitus, nystagmus, nausea and vomiting.

Peripheral circulatory disorders

• Maintenance therapy for symptoms of peripheral circulatory disorders, including Raynaud’s phenomenon, acrocyanosis, intermittent claudication, trophic disturbances, trophic and varicose ulcers, paraesthesia, nocturnal cramps, cold extremities.

Motion sickness

• Prophylaxis of motion sickness.

Dosage and Administration

Dosage

Cerebral circulatory disorders – Adults

• 1 tablet of 25 mg three times a day.

Disorders of balance – Adults

• 1 tablet of 25 mg three times a day.

Peripheral circulatory disorders – Adults

• 2 to 3 tablets of 25 mg three times a day. The maximum recommended dosage should not exceed 225 mg daily.

Motion sickness

• Adults and adolescents aged 13 years and above: 1 tablet of 25 mg at least half an hour before travelling; to be repeated every 6 hours.

• Children aged 6 to 12 years: half of the adult dose is recommended.

Administration

STUGERON® should preferably be taken after meals.

Contraindications

STUGERON® is contraindicated in patients with known hypersensitivity to the drug.

Warnings and Precautions

As with other antihistamines STUGERON® may cause epigastric distress; taking it after meals may diminish gastric irritation.

In patients with Parkinson’s disease STUGERON® should only be given if the advantages outweigh the possible risk of aggravating this disease. STUGERON® may cause somnolence, especially at the start of treatment. Therefore caution should be taken when alcohol, central nervous system (CNS) depressants or tricyclic antidepressants are used concomitantly.

Interactions

Alcohol, CNS depressants and tricyclic antidepressants

The sedative effects of STUGERON® and of any of the following may be potentiated when used concomitantly: alcohol, CNS depressants, or tricyclic antidepressants.

Diagnostic interference

Because of its antihistamine effect, STUGERON® may prevent otherwise positive reactions to dermal reactivity indicators if used up to 4 days prior to skin testing.

Pregnancy and Breast-feeding

Pregnancy

Although in animal studies STUGERON® has shown no teratogenic effects, as with all drugs, STUGERON® should be used during pregnancy only if the therapeutic benefits justify the potential risks for the fetus.

Breast-feeding

There are no data on the excretion of STUGERON® in human breast milk: nursing should therefore be discouraged in women using STUGERON®.

Effects on Ability to Drive and Use Machines

Since somnolence may occur, especially at the start of treatment, caution should be taken during activities such as driving or operating machinery.

Adverse Reactions

Throughout this section, adverse reactions are presented. Adverse reactions are adverse events that were considered to be reasonably associated with the use of cinnarizine based on the comprehensive assessment of the available adverse event information. A causal relationship with cinnarizine cannot be reliably established in individual cases.

Further, because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

Clinical trial data

Placebo-controlled double-blind data — adverse reactions reported at ≥1% incidence

The safety of STUGERON® (30 to 225 mg/day) was evaluated in 740 subjects (of which 372 were treated with STUGERON®, 368 were given placebo) who participated in 7 placebo-controlled, double-blind clinical trials: three in the treatment of peripheral circulatory disorders, one in the treatment of cerebral circulatory disorders, two in vertigo, and one in seasickness.

Adverse reactions reported by ≥1% of STUGERON® treated subjects noted in the double-blind clinical trials are shown in Table 1.

Table 1. Adverse Reactions Reported by ≥1 % of STUGERON®-treated Subjects in 7 Double-Blind Placebo-Controlled Clinical Trials of STUGERON®

System/Organ Class
Preferred Term
STUGERON® (n=372)
%
Placebo
(n=368)
%
Nervous System Disorders

Somnolence

8.3 4.6

Comparator and open-label data – adverse reactions reported at ≥1% incidence

Six comparator trials and thirteen open label trials were selected to determine the incidence of adverse reactions. In these 19 studies, 668 subjects were treated with doses ranging from 50 to 225 mg/day STUGERON@, in the treatment of peripheral circulatory disorders, cerebral circulatory disorders, and vertigo.

Adverse reactions reported by ≥1% of STUGERON® treated subjects noted in the comparator and open-label clinical trials are shown in Table 2.

Table 2. Adverse Reactions Reported by ≥1% of STUGERON®-treated Subjects in 6 Comparator and 13 Open-Label Clinical Trials of STUGERON®

System/Organ Class
Preferred Term
STUGERON® (n=668)
%
Gastrointestinal Disorders

Nausea

1.5
Investigations

Weight increased

2.1

Placebo, comparator, and open-label data – adverse reactions reported at <1% incidence

Additional adverse reactions that occurred in <1% of STUGERON® treated subjects in the above 2 clinical datasets are listed below in Table 3.

Table 3. Adverse Reactions Reported by <1% of STUGERON®-treated Subjects in Either the Placebo- or Comparator-controlled or Open Clinical Trials.

Nervous System Disorders

Hypersomnia

Lethargy

Gastrointestinal Disorders

Stomach discomfort

Vomiting

Abdominal pain upper

Dyspepsia

Skin and Subcutaneous Tissue Disorders

Hyperhidrosis

General Disorders and Administration Site Conditions

Fatigue

Postmarketing data

Adverse events first identified as adverse reactions during postmarketing experience with cinnarizine are included in Table 4.

The postmarketing review was based on review of all cases where there was a use of cinnarizine. In Table 4, adverse reactions are presented by frequency category based on spontaneous reporting rates, with frequencies provided according to the following convention:

Very common ≥1/10

Common ≥1/100 to <1/10

Uncommon ≥1/1000 to <1/100

Rare ≥1/10000 to <1/1000

Very rare <1/10000 including isolated reports

Table 4. Adverse Reactions Identified During Postmarketing Experience with cinnarizine (STUGERON®) by Frequency Category Estimated From Spontaneous Reporting Rates

System/Organ Class
Preferred Term
Frequency
Nervous System Disorders
Dyskinesia Very rare
Extrapyramidal disorder Very rare
Parkinsonism Very rare
Tremor Very rare
Skin and Subcutaneous Tissue Disorders
Lichenoid keratosis Very rare
Lichen planus Very rare
Subacute cutaneous lupus erythematosus Very rare
Musculoskeletal, Connective Tissue and Bone Disorders
Muscle rigidity Very rare

Overdose

Symptoms and signs

Acute cinnarizine overdoses have been reported with doses ranging from 90 to 2250 mg.

The most commonly reported signs and symptoms associated with overdose of cinnarizine include: alterations in consciousness ranging from somnolence to stupor and coma, vomiting, extrapyramidal symptoms, and hypotonia. In a small number of young children, seizures developed. Clinical consequences were not severe in most cases, but deaths have been reported after single and polydrug overdoses involving cinnarizine.

Treatment

There is no specific antidote. For any overdose, the treatment is symptomatic and supportive care. Activated charcoal may be given if considered appropriate.

PHARMACOLOGICAL PROPERTIES

Pharmacodynamic Properties

Pharmacotherapeutic group: antivertigo preparations, ATC code: N07CA02.

Cinnarizine has an anti-histamine (H1)-effect.

Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking calcium channels.

In addition to this direct calcium antagonism, cinnarizine decreases the contractile activity of vasoactive substances, such as norepinephrine and serotonin, by blocking receptor-operated calcium channels. Blockade of the cellular influx of calcium is tissue-selective, and results in antivasoconstrictor properties without effect on blood pressure and heart rate.

Cinnarizine may further improve deficient microcirculation by increasing erythrocyte deformability and decreasing blood viscosity. Cellular resistance to hypoxia is increased.

Cinnarizine inhibits stimulation of the vestibular system, which results in suppression of nystagmus and other autonomic disturbances. Acute episodes of vertigo can be prevented or reduced by cinnarizine.

Pharmacokinetic Properties

Absorption

The peak plasma levels of cinnarizine are obtained 1 to 3 hours after intake.

Distribution

The plasma protein binding of cinnarizine is 91%.

Metabolism

Cinnarizine is extensively metabolized mainly via CYP2D6.

Elimination

The reported elimination half-life for cinnarizine ranges from 4 to 24 hours. The elimination of metabolites is about 1/3 in the urine and 2/3 in the feces.

NON-CLINICAL INFORMATION

A comprehensive battery of nonclinical safety studies showed that effects were observed only after chronic exposures from approximately 5 to 72 times, on a mg/kg basis when compared to the maximum recommended human dose of 225 mg/day, calculated as 4.5 mg/kg as based on a 50 kg person.

PHARMACEUTICAL INFORMATION

List of Excipients

25mg tablets: Cotton seed oil hydrogenated, lactose monohydrate, maize starch, polyvidone. Sucrose, talc.

Incompatibilities

None known.

Shelf Life

See expiry date on the outer pack.

Storage Conditions

See storage conditions on the outer pack.

Keep out of reach of children.

Nature and Contents of Container

Blister packs.

Instructions for Use and Handling

No special requirements.

Instructions for Disposal

Any unused product or waste material should be disposed of in accordance with local requirements.

MANUFACTURED BY

See outer carton.

DATE OF REVISION OF THE TEXT

18 March 2013

© Janssen-Cllag 2013

Teva Metoprolol Tartrate Tablets

METOPROLOL TARTRATE 50 mg AND 100 mg TABLETS

PACKAGE LEAFLET: INFORMATION FORTHE USER

 

Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.

• Keep this Ieaflet. You may need to read it again.

• If you have any further questions, ask your doctor, pharmacist or nurse.

• This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.

• If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this leaflet. See section 4.

 

What is in this leaflet

1 What Metoprolol is and what it is used for

2 What you need to know before you take Metoprolol

3 How to take Metoprolol

4 Possible side effects

5 How to store Metoprolol

6 Contents of the pack and other information

 

1 What Metoprolol is and what it is used for

Metoprolol belongs to a group of drugs called beta-blockers, which affect the heart and circulation.

Metoprolol tablets are used to:

• Manage high blood pressure

• Manage angina pectoris (chest pain) and heartbeat irregularities, and may also be given after a heart attack

• Prevent recurrent migraines

• Treat hyperthyroidism (an overactive thyroid gland).

 

2 What you need to know before you take Metoprolol

Do NOT take Metoprolol if you

• Are allergic to metoprolol tartrate or any of the other ingredients of this medicine (listed in section 6)

• Are allergic to any other beta-blocker drugs

• Have severe asthma or severe attacks of wheezing

• Have heart failure, severe slow heart beat, irregular heart beat, narrowing of the arteries or had a heart attack with complications

• Have second or third degree heart block (a condition which may be treated by a
pacemaker)

• Have low blood pressure

• Have poor circulation

• You been told that you have high blood pressure due to a tumour near your kidney (phaeochromocytoma)

• Are pregnant or breast-feeding

• Have metabolic acidosis (a condition where there is a change in the acid/base balance of the body).

 

Warnings and precautions

Talk to your doctor or pharmacist or nurse before taking Metoprolol. If you:

• Have a history of or suffer from allergies

• Have any other heart problems, in particular, a slow heartbeat

• Have poor blood circulation or controlled heart failure

• Suffer from psoriasis (patches of thickened and sore skin)

• Are diabetic. Your treatment for diabetes may need to be adjusted

• Have any liver problems

• Have a history of asthma or wheezing or any similar lung disorder

• Have recently suffered a severe allergic reaction

• Have a tumour of the adrenal gland (phaeochromocytoma)

• Have a type of chest pain (angina) called prinzmetal’s angina

• Have first degree heart block

• Have thyrotoxicosis (a condition caused by an overactive thyroid gland).Your medicine may hide the symptoms of thyrotoxicosis.

• Suffer from eye disorders.

If you are about to undergo surgery requiring anaesthetic, tell your doctor or dentist that you are taking Metoprolol.

 

Other medicines and Metoprolol

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines of the following:

• Clonidine (for high blood pressure or migraine). If you are taking clonidine and metoprolol together, do not stop taking clonidine unless your doctor has told you to do so. If you have to stop taking clonidine or metoprolol, your doctor will give you careful instructions about how to do it.

• Other drugs for your heart or to reduce blood pressure, e.g. prazosin

• Other beta blockers, e.g. timolol, for glaucoma

• Monoamine-oxidase inhibitors, for depression, e.g. phenelzine

• Verapamil, diltiazem, hydralazine, nifedipine (used to treat heart problems)

• Quinidine, amiodarone (for heart problems)

• Cimetidine (used to treat heartburn)

• Cardiac glycosides e.g. digoxin (used to treat heart failure)

• Rifampicin (used to treat tuberculosis)

• Lidocaine (used as a local anaesthetic to relieve pain)

• Ergotamine (used to treat migraine)

• Medicines to treat other mental illnesses (such as phenothiazines)

• Antiretroviral drugs (e.g. ritonavir) used to treat AIDS and some other conditions

• Drugs to prevent malaria

• Medicines to treat fungal infections

• Adrenaline (used in emergency treatment e.g. allergic reactions)

• Indometacin and celecoxib (used to treat inflammation of the joints, gout and period pain) medicines for the treatment of diabetes (including insulin).Your doctor may need to adjust your dose of these medicines.

Tell your doctor or pharmacist if you are taking, have recently taken or might take other medicines, including medicines obtained without a prescription.

 

Taking Metoprolol with food, drink and alcohol

You should keep your alcohol intake to a minimum while you are taking Metoprolol, as alcohol may increase the effect of this drug.

 

Pregnancy, breast-feeding and fertility

If you are pregnant, or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.

 

Driving and using machines

Metoprolol may cause dizziness and tiredness, if affected do not drive or operate machinery.

 

Metoprolol contains Lactose monohydrate

Patients who are intolerant to lactose should note that Metoprolol Tablets contain a small amount of lactose. If you have been told by your doctor that you have an intolerance to some sugars, contact your doctor before taking this medicinal product.

 

3 How to take Metoprolol

Always take this medicine exactly as your doctor or pharmacist has told you. Check with your doctor, pharmacist or nurse if you are not sure. The tablets should be swallowed preferably with a glass of water. Metoprolol can be taken with or without food.

The recommended dose is:

Adults

High blood pressure

Initially 100 mg/day in the morning, which may be increased to a maximum of 400 mg daily.

Your doctor may combine this dose with a diuretic (water tablet) or another blood
pressure-lowering drug.

 

Angina

50 to 100 mg two or three times daily.

 

Irregular heartbeat

50 mg two or three times daily. If necessary this may be increased to 300 mg/day in divided doses.

 

Hyperthyroidism

50 mg four times daily. Your doctor may reduce the dosage as your condition improves.

 

Heart attack

The usual maintenance dose following a heart attack is 200 mg daily.

 

Migraine prevention

100 to 200 mg/day in divided doses.

 

Patients with liver problems

A reduced dose may be necessary.

 

Older people

A reduced dose may be necessary.

 

Use in children and adolescents

Metoprolol tablets are not recommended for use in children.

 

If you take more Metoprolol than you should

If you (or someone else) swallow a lot of the tablets all together, or if you think a child has swallowed any of the tablets, contact your nearest hospital casualty department or your doctor immediately. An overdose is likely to cause low blood pressure (feeling dizzy or faint), a slow heartbeat, your heart may suddenly stop, difficulty breathing, reduced consciousness, feeling sick, being sick, blue discolouration of skin and coma. Please take this leaflet, any remaining tablets and the container with you to the hospital or doctor so that they know which tablets were consumed.

 

If you forget to take Metoprolol

If you forget to take a tablet, take one as soon as you remember, unless it is nearly time to take the next one. Do not take a double dose to make up for a forgotten tablet dose.

Take the remaining doses at the correct time.

 

If you stop taking Metoprolol

You should continue to take these tablets for as long as your doctor tells you to.

DO NOT stop taking your medicine without talking to your doctor first, even if you feel better. Your treatment with Metoprolol must not be stopped suddenly. If it is necessary to stop treatment, your doctor should reduce your dose gradually.

If you have any further questions on the use of this medicine, ask your doctor, pharmacist or nurse.

 

4 Possible side effects

Like all medicines, this medicine can cause side effects, although not everybody gets them.

If the following happens, stop taking the tablets and tell your doctor immediately or go to the casualty department at your nearest hospital:

• An allergic reaction (swelling of the lips, face or neck leading to severe difficulty in breathing; skin rash or hives).

This is a very serious but rare side effect. You may need urgent medical attention or hospitalisation.

 

The side effects listed below have been reported.

Common (may affect up to 1 in 10 people)

• Headache, dizziness, or unusual tiredness

• Slow heart beat

• Low blood pressure which might make you faint or dizzy

• Feeling short of breath when exercising

• Feeling or being sick, stomach ache

 

Rare (may affect up to 1 in 1,000 people)

• Depression

• Sleep disorders such as sleepiness, difficulty in sleeping or nightmares

• Feeling less alert

• Coldness, numbness or tingling in your hands and feet

• Muscle cramps

• Heart problems which can cause shortness of breath or ankle swelling (heart failure) or irregular heart beat or a very fast, uneven or forceful heartbeat

• Water retention (oedema)

• Poor blood circulation which makes the toes and fingers numb and pale (Raynaud’s phenomenon)

• Breathlessness or wheeziness (bronchospasm)

• Diarrhoea or constipation

• Skin rash (including nettle rash, patches of thickened and sore skin) and/or itching.

 

Very rare (may affect up to 1 in 10,000 people)

• Reduction in blood platelets, which increases risk of bleeding or bruising

• Weight gain

• Hallucinations or personality disorders

• Dry or sore eyes or problems with vision

• Ringing in the ears (tinnitus) or partial loss of hearing or deafness (hearing problems)

• Gangrene

• Runny and itchy nose (rhinitis), dry mouth

• Changes in the results of liver function tests

• Bruising or increased sensitivity of the skin to sunlight, worsening of patches of thickened and sore skin (psoriasis)

• Increased sweating, loss of hair (alopecia)

• Impotence or loss of libido

• Painful joints

• Chest pain.

 

Frequency not known (cannot be estimated from the available data)

• Confusion

• Abnormal levels of certain types of fats such as cholesterol or triglycerides in the blood

• Abnormal curvature of the penis with painful erections (known as Peyronie’s disease)

• Retroperitoneal fibrosis where abnormal scar tissue occurs behind the membrane that lines the cavity of the abdomen. This may present with pain in the back, groin or the lower abdomen

• Hepatitis

• Positive anti-nuclear antibodies (an indicator of autoimmune disease where the body attacks its own tissues)

• Memory loss, nervousness, anxiety, taste disturbance

• Conjunctivitis

• An increase in intermittent claudication (a cramp-like pain brought on by exercise).

If any of the side effects get serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.

 

Reporting of side effects

If you get any side effects, talk to your doctor, pharmacist or nurse. This includes any possible side effects not listed in this Ieaflet. You can also report side effects directly via the Yellow Card Scheme at: http://www.mhra.gov.uk/yellowcard. By reporting side effects you can help provide more information on the safety of this medicine.

 

5 How to store Metoprolol

Keep out of the sight and reach of children.

Do not store above 25°C.

Do not use this medicine after the expiry date which is stated on the outer packaging. The expiry date refers to the last day of that month.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help to protect the environment.

 

6 Contents of the pack and other information

What Metoprolol Tablets contain

• The active ingredient is metoprolol tartrate.

• The other ingredients are microcrystalline cellulose (E460), lactose monohydrate, sodium starch glycolate, colloidal anhydrous silica and magnesium stearate.

 

What Metoprolol Tablets look like and contents of the pack

• The 50 mg tablets are round, biconvex white tablets, engraved ‘4A5’ with a breakline on the reverse.

• The 100 mg tablets are round, biconvex white tablets, engraved ‘4A6’ with a breakline on the reverse.

• The product is available in pack sizes of 28, 30, 56, 60, 100, 500 tablets.

Not all pack sizes may be marketed.

 

Marketing Authorisation Holder and Manufacturer

Marketing Authorisation holder and company responsible for manufacture:

TE VA UK Limited, Eastbourne, BN22 9AG

 

This leaflet was last revised: January 2015
PL 00289/0743-0744

Diclopac Diclofenac Potassium Tablets

DICLOPAC

Diclofenac Potassium Tablets

 

1 NAME OF THE MEDICINAL PRODUCT

DICLOPAC 50mg film coated tablets.

 

2 QUALITATIVE AND QUANTITATIVE COMPOSITION

Each film coated tablet contains:

Diclofenac Potassium BP: 50mg

Excipients: Q.S.

Colour: Red Oxide of Iron & Titanium Dioxide

 

3 PHARMACEUTICAL FORM

Tablet.

For oral administration.

 

4 CLINICAL PARTICULARS

4.1 Therapeutic indications

DICLOPAC is indicated for the short-term treatment of all grades of pain and inflammation in the following acute conditions:

Post-traumatic pain, inflammation and swelling, e.g. due to sprains.

Acute musculo-skeletal disorders such as periarthritis (for example frozen shoulder), tendonitis, tenosynovitis, bursitis.

Postoperative pain, inflammation and swelling, e.g. following dental or orthopaedic surgery.

Painful and/or inflammatory conditions in gynaecology, e.g. primary dysmenorrhoea or anxiety and associated menorrhagia.

Migraine attacks.

Acute gout.

Painful syndromes of the vertebral column.

Non-articular rheumatism.

As an adjuvant in severe painful inflammatory infections of the ear, nose or throat, e.g. pharyngotonsillitis, otitis. In keeping with general therapeutic principles, the underlying disease should be treated with basic therapy, as appropriate. Fever alone is not an indication.

 

4.2 Posology and method of administration

Adults

The recommended initial daily dose is 100 to 150mg. In milder cases, 75 to 100 mg daily is usually sufficient. The total daily dose should generally be divided in 2 to 3 doses.

 

4.3 Contraindications

Known hypersensitivity to the active substance or to any of the excipients.

History of gastrointestinal bleeding or perforation, related to previous NSAIDs therapy.

Active or history of recurrent peptic ulcer/ haemorrhage (two or more distinct episodes of proven ulceration or bleeding).

Last trimester of pregnancy.

Severe hepatic, renal and heart failure.

Like other non-steroidal anti-inflammatory drugs (NSAIDs) it is also contraindicated in patients in whom attacks of asthma, urticaria, or acute rhinitis are precipitated by acetylsalicylic acid or other NSAIDs.

 

4.4 Special warnings and precautions for use

Warnings

Gastrointestinal bleeding or ulceration or perforation, which can be fatal, have been reported with all NSAIDs, including diclofenac, and may occur at any time during treatment, with or without warning symptoms or a previous history of serious gastrointestinal events. The elderly have an increased frequency of adverse reactions to NSAIDs especially gastrointestinal bleeding and perforation which may be fatal. When gastrointestinal bleeding or ulceration occurs in patients receiving diclofenac, the medicinal product should be withdrawn.

 

Precautions

Undesirable effects may be minimized by using the lowest effective dose for the shortest possible duration necessary to control symptoms.

The use of DICLOPAC with concomitant NSAIDs including cyclooxygenase-2 selective inhibitors, should be avoided due to the absence of any evidence demonstrating synergistic benefits and the potential for additive undesirable effects.

Caution is indicated in the elderly on basic medical grounds. In particular it is recommended that the lowest effective dosage be used in frail elderly patients or those with a low body weight.

 

4.5 Interaction with other medicinal products and other forms of interaction

The following interactions include those observed with diclofenac potassium.

Lithium: If used concomitantly, diclofenac may raise plasma concentrations of lithium. Monitoring of the serum lithium level is recommended.

Digoxin: If used concomitantly, diclofenac may raise plasma concentrations of digoxin. Monitoring of the serum digoxin level is recommended.

Diuretics and antihypertensive agents: Like other NSAIDs, concomitant use of diclofenac with diuretics or antihypertensive agents (e.g. beta-blockers, angiotensin converting enzyme (ACE) inhibitors) may cause a decrease in their antihypertensive effect. Therefore, the combination should be administered with caution and patients, especially the elderly, should have their blood pressure periodically monitored. Patients should be adequately hydrated and consideration should be given to monitoring of renal function after initiation of concomitant therapy and periodically thereafter, particularly for diuretics and ACE inhibitors due to the increased risk of nephrotoxicity. Concomitant treatment with potassium-sparing drugs may be associated with increased serum potassium levels, which should therefore be monitored frequently.

 

4.6 Pregnancy and lactation

Pregnancy

The use of diclofenac in pregnant women has not been studied. Therefore, DICLOPAC should not be used during the first two trimesters of pregnancy unless the potential benefit to the mother outweighs the risk to the foetus. As with other NSAIDs, use of diclofenac during the third trimester of pregnancy is contraindicated owing to the possibility of uterine inertia and/or premature closure of the ductus arteriosus.

Lactation

Like other NSAIDs, diclofenac passes into the breast milk in small amounts. Therefore it should not be administered during breast feeding in order to avoid undesirable effects in the infant.

 

4.7 Undesirable effects

If serious side-effects occur, Diclofenac Potassium tablets should be withdrawn.

Gastrointestinal: The most commonly-observed adverse events are gastrointestinal in nature. Peptic ulcers, perforation or GI bleeding, sometimes fatal, particularly in the elderly, may occur. Nausea, vomiting, diarrhoea, flatulence, constipation, dyspepsia, abdominal pain, melaena, haematemesis, ulcerative stomatitis, exacerbation of colitis and Crohn’s disease have been reported following administration. Less frequently, gastritis has been observed. Pancreatitis has been reported very rarely.

Hypersensitivity: Hypersensitivity reactions have been reported following treatment with NSAIDs. These may consist of (a) non-specific allergic reactions and anaphylaxis (b) respiratory tract reactivity comprising asthma, aggravated asthma, bronchospasm or dyspnoea, or (c) assorted skin disorders, including rashes of various types, pruritus, urticaria, purpura, angiodema and, more rarely exfoliative and bullous dermatoses (including epidermal necrolysis and erythema multiforme).

 

4.8 Overdose

Symptoms

There is no typical clinical picture resulting from diclofenac overdosage. Overdosage can cause symptoms such as vomiting, gastrointestinal haemorrhage, diarrhoea, dizziness, tinnitus or convulsions. In the event of significant poisoning, acute renal failure and liver damage are possible.

Therapeutic measures

Management of acute poisoning with NSAIDs, including diclofenac, essentially consists of supportive measures and symptomatic treatment. Supportive measures and symptomatic treatment should be given for complications such as hypotension, renal failure, convulsions, gastrointestinal disorder, and respiratory depression.

 

5 PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Diclofenac Potassium tablets contain the potassium salt of diclofenac, a non-steroidal compound with pronounced and clinically demonstrable analgesic, anti-inflammatory and anti-pyretic properties.

Diclofenac is a potent inhibitor of prostaglandin biosynthesis and a modulator of arachidonic acid release and uptake.

Diclofena Potassium tablets have a rapid onset of action and are therefore suitable for the treatment of acute episodes of pain and inflammation.

In migraine attacks Diclofenac Potassium tablets have been shown to be effective in relieving the headache and in improving the accompanying symptom of nausea.

Diclofenac in vitro does not suppress proteoglycan biosynthesis in cartilage at concentrations equivalent to the concentrations reached inhuman beings.

 

5.2 Pharmacokinetic properties

Absorption

Diclofenac is rapidly and completely absorbed from sugar coated tablet. Food intake does not affect absorption. Peak plasma concentration after one 50 mg sugar-coated tablet was 3.9 µmol/l after 20-60 minutes. The plasma concentrations show a linear relationship to the size of the dose.

Diclofenac undergoes first-pass metabolism and is extensively metabolised.

Distribution

Diclofenac is highly bound to plasma proteins (99.7%), chiefly albumin (99.4%).

Biotransformation

The biotransformation of diclofenac involves partly glucuronidation of the intact molecule but mainly single and multiple hydroxylation followed by glucuronidation.

Elimination

The total systemic clearance of diclofenac in plasma is 263 ± 56 ml/min (mean ± SD). The terminal half-life in plasma is 1 – 2 hours. Repeated oral administration of Diclofenac Potassium tablets for 8 days in daily doses of 50 mg t.d.s does not lead to accumulation of diclofenac in the plasma. Approx. 60% of the dose administered is excreted in the urine in the form of metabolites, and less than 1% as unchanged substance. The remainder of the dose is eliminated as metabolites through the bile in the faeces.

 

6 PHARMACEUTICAL PARTICULARS

6.1 Shelf life

48 months

 

6.2 Special precaution for storage

Do not store above 3 0°C. Keep in the original container and protect from light.

KEEP OUT OF REACH OF CHILDREN

 

6.3 Presentation

10 blister pack of 10 tablets in 1 pack.

 

7 MARKETING AUTHORISATION HOLDER

Manufactured in India by

Saga Laboratories

Survey No. 198/2 & 198/3, Chachrawadi Vasna,

Tal.: Sanand, Dist.: Ahmedabad 382 210, India.

 

Manufactured for

MEDITRADE Nig. Limited

3, Salawu Street OIodi Apapa, Lagos, Nigeria.

 

Marketed by

GreenPeck Nigeria Limited

54, Oyewole Street, Palm-Grove Estate

Lagos, Nigeria

greenpecknigltd@yahoo.com

 

8.MARKETING AUTHORISATION NUMBER(S)

Mfg. Lic. No.: G/25/1877

Artwork No.: 5459101-02