Acinil Omeprazole Capsules

ACINIL Capsules 20 mg

OMEPRAZOLE CAPSULE BP

For the use only of a Registered Medical Practitioner or a Hospital or a Laboratory.

 

COMPOSITION

Each hard gelatin Capsule contains:

Omeprazole B.P. 20mg

(As enteric coated pellets)

Approved colours used in capsule shell.

 

INDICATIONS

Omeprazole is indicated in the treatment of:

• Duodenal Ulcer.

• Gastric Ulcer.

• Zollinger-Ellison syndrome.

• Reflux oesophagitis

If duodenal ulcers are associated with Helicobacter pylori, the concomitant use of omeprazole and suitable antibiotics may be beneficial.

 

DOSAGE AND ADMINISTRATION

A daily 20 mg dose is recommended for treatment of duodenal and gastric ulcer and reflux oesophagitis. 40 mg/day may be required in patients with conditions poorly responsive to histamine H2 receptor antagonist therapy.

Recurrence of reflux oesophagitis has been successfully prevented with daily 20 or 40mg dose while a 10 mg daily dose appears promising in patients with duodenal ulcer.

In patients with Zollinger-Ellison syndrome, omeprazole 60 mg/day is recommended initially with individual adjustment to maintain target gastric acid output.

Dosage adjustment is not necessary in elderly patients or in patients with renal or hepatic impairment.

 

CONTRAINDICATIONS

Hypersensitivity to any of the ingredients in this product.

 

WARNINGS AND PRECAUTIONS

Decreased gastric acidity due to any means, including proton-pump inhibitors, increases gastric counts of bacteria normally present in the gastrointestinal tract. Treatment with acid-reducing drugs may lead to a slightly increased risk of gastrointestinal infections, such as Salmonella and Campylobacter.

For severely ill children, who require long-term treatment with Omeprazole, and may have borderline levels or body stores of B12, it may be advisable to monitor serum B12 levels during long-term treatment.

 

DRUG INTERACTIONS

Omeprazole can prolong the elimination of medicines which are metabolised by oxidation in the liver, e.g. warfarin, diazepam and phenytoin.

Patients receiving warfarin or phenytoin concomitant with omeprazole, should be monitored closely as a reduction in dosages of warfarin or phenytoin may be required.

It was however shown in patients on concurrent omeprazole treatment at a daily dosage of 20 mg and continuous phenytoin treatment, that the simultaneous use of these two medications did not influence the blood concentration of phenytoin. Concomitant treatment with omeprazole 20 mg daily also did not alter coagulation time in patients on long-term treatment.

There is a possibility of interactions with medicines metabolised via the cytochrome P450 enzyme system, although no interactions with propranolol, metoprolol, theophylline, lignocaine, quinidine and amoxycillin have been recorded.

No interaction with food or the concurrent administration of antacid medications has been found. The plasma concentrations of both omeprazole and clarithromycin may be increased during concomitant treatment with these medicines.

An increase of approximately 10% in the bioavailability of digoxin were recorded in healthy volunteers due to the increase in intragastric pH when omeprazole and digoxin are administered concurrently.

 

PREGNANCY AND LACTATION

Safety in pregnancy and lactation has not been established.

 

UNDESIRABLE EFFECTS

The most commonly reported side effects are Nausea, vomiting, headache, diarrhoea, constipation, abdominal pain and flatulence, rash and/or pruritis, dizziness, paraesthesia, somnolence, insomnia, vertigo, increased liver enzymes and malaise.

 

PHARMACOLOGICAL ACTION

Omeprazole is a specific inhibitor of the gastric proton pump in the parietal cell and thus reduces the secretion of gastric acid. Reversible control of gastric acid secretion is produced with single daily doses of omeprazole. Omeprazole is a weak base, which is concentrated in the intracellular canaliculi of the parietal cell. Due to the acidic environment in these cells, omeprazole is converted to the active form, where it acts as an inhibitor of the enzyme H+, K+ -ATPase – the proton pump. There is a dose dependency on this final step in the formation of gastric acid, which provides for effective inhibition of the secretion of both basal acid and stimulated acid irrespective of the secretatory enhancer.

When omeprazole is given daily as a single oral dose, the gastric acid secretion is inhibited with a maximum effect reached within four days of treatment. In patients with duodenal ulcers, a mean decrease of approximately 80% in intragastric acidity is then maintained over a 24-hour period, with the mean decrease in peak acid output after pentagastrin stimulation being approximately 70%, twenty-four hours after initiating treatment with omeprazole.

 

PHARMACOKINETICS

Due to the acid liability of omeprazole, the oral formulation consists of enteric-coated granules in capsules. Omeprazole is usually completely absorbed from the small intestine within three to six hours.

After a single oral dose the systemic bioavailability of omeprazole is approximately 35% which can be increased to about 60%, after repeated once-daily administration.

The simultaneous intake of food has no influence on the bioavailability. Omeprazole is approximately 95% bound to plasma proteins.

The average terminal phase half-life of the plasma concentration-time curve is approximately forty minutes. There is no change in half-life during treatment. The inhibition of acid secretion is related to the area under the plasma concentration-time curve (AUC) and not to the actual plasma concentration at a given time.

Omeprazole is completely metabolised mainly in the liver. The sulphone, the sulphide and hydroxy omeprazole are the metabolites detected in plasma. These metabolites are inactive and have no significant effect on acid secretion.

Approximately 80% of the metabolites are excreted in the urine and the balance in the faeces. The two main metabolites in the urine are hydroxy-omeprazole and the corresponding carboxylic acid.

There is no significant change in the systemic bioavailability of omeprazole in patients with impaired renal function.

Although the area under the plasma concentration-time curve is increased in patients with reduced liver function, no apparent accumulation of omeprazole has been found.

 

STORAGE

Store below 25oC, protect from light and moisture.

 

PRESENTATION

2 strips containing 10 capsules each are packed in 5 primary carton along with the Pack Insert.

 

KEEP OUT OF REACH OF CHILDREN.

Carefully read the accompanying instructions before use.

 

Marketed by

PHILLIPS PHARMACEUTICALS NIGERIA LIMITED

Plot 122-132 Apapa-Oshodi Expressway,

lyana-Isolo Lagos Nigeria.

 

Manufactured by

AGIO PHARMACEUTICALS LTD.

A-38, Nandjyot Industrial Estate,

Kurla-Andheri Road, Safedpool,

Mumbai-400 072 India.

At:T-82, M.I.D.C., Bhosari, Pune-411026.

Kriscet Cimetidine USP Caplets

KRISCET-400

CIMETIDINE USP 400MG CAPLETS

Please read right through this leaflet before you start using this medicine.

Kriscet-400 caplets (Cimetidine USP 400mg caplets) belong to a group of medicines called H2-receptor antagonists which act to decrease the natural production of acid in the stomach.

 

1. KRISCET-400 HAVE BEEN PRESCRIBED TO TREAT ANY OF THE FOLLOWING

Ulcers in the stomach or duodenum which may be caused by non-steroidal anti-inflammatory drugs (NSAIDs OFTEN USED TO REDUCE PAIN, FEVER AND INFLAMATION).

Acid from the stomach escaping into the fluid pipe causing pain, inflamation and heartburn (easophageal reflux disease).

Excess acid in the stomach caused by a tumor in the pancreas (Zolinger- Elison syndrome).

Various conditions where reduction of gastric by cimetidine has been shown to be beneficial e.g.

• Indigestion symptoms (e.g. stomach pain or discomfort, heartburn)

• Meal-related upper abdominal pain,

• To prevent stress ulcers from bleeding,

• To be given before general anaesthesia to prevent damage to the lungs caused by breathing in stomach fluids (acids aspiration),

• To improve absorption of food and reduce fluid loss in short bowel syndrome,

• Reduction of breakdown of pancreatic enzyme supplements.

 

2. BEFORE YOU TAKE KRISCET-400

Consult your doctor before taking Kriscet-400:

• If you suffer or have suffered in the past from kidney or liver disease.

• If you have a history of peptic ulcer; particularly if you are taking a non-steroidal anti-Inflammatory drug (NSAID) e.g. Asprin, Ibuprofen, Naproxen, Diclofenac.

• If you are taking drugs or you have an illness that could cause a fall in blood cell count.

• If you are middle aged or over; with new or recently changed indigestion symptoms (e.g. stomach pain or discomfort, heartburn), other causes of your symptoms such as stomach cancer, should be excluded.

 

Pregnancy

Ask your doctor for advice before taking Kriscet-400 if you are pregnant or trying to become pregnant or if you are breastfeeding.

 

Taking other medicines

Please inform your doctor or pharmacist if you are taking or have recently taken any other medicines even those not prescribed

• Anticoagulants (to thin your blood) e.g. warfarin.

• Anticonvulsants (to prevent fits) e.g. phenytoxin.

• Bronchodilators (for breathing difficulties) e.g. theophylline.

• Anti-arrhythmics (to slow heart rate) e.g. indocaine.

• Immunodepressants (to prevent transplant rejection) e.g. cyclosporine.

 

3. HOW TO TAKE KRISCET-400

The usual dosage is 400mg to 160mg per day, in divided doses. Do not take more that 2400mg per day. If you suffer from kidney or liver problems, you may require a lower dose. The usual duration of treatment is 4-8 weeks. The tablets should be taken with meals and at bedtime and swallowed whole with a glass of water. Unless specifically directed by your physician. In the event of an accidental overdose, contact your nearest hospital’s casualty department or tell your doctor immediately. Take your tablet pack with you.

 

4. POSSIBLE SIDE EFFECTS

Like all medicines, kriscet-400 cause side effects, although not everybody gets them.

Allergic reactions may occur rarely, with symptoms such as rash, itching, swelling of the face, wheeziness, shortness of breath, tightness in the chest, fever, low blood pressure and feeling dizzy particularly when standing up. If any of these occur STOP taking the medicine and contact a doctor immediately.

Side effects that have been reported: diarrhea, skin rash, tiredness, breast enlargement in men, hair loss and confusion.

Hallucination, liver disorders (characterized mainly by sore throat, ulcers in the mouth and throat, unusual tiredness or weakness, unusual bleeding, unexplained bruises).

Many of the above mentioned side effects should disappear when treatment is stopped.

Tell your doctor if you have any other unwanted side effect not mentioned above.

 

5. STORAGE

Do not store above 25oC. Keep out of reach and sight of children.

 

6. FURTHER INFORMATION

PRESENTATION

CAPLETS: 1 X 2O CAPLETS

 

NAFDAC REG. NO: A4-9283

 

Manufactured by

KRISHAT PHARMA IND. LTD.

9 Kilometer, Old Lagos Road,

Podo Ibadan, Nigeria.

http://www.krishapharm.com

Cytotec Misoprostol 200 microgram Tablets

Cytotec®
Misoprostol 200 microgram Tablets

 

1. NAME OF THE MEDICINAL PRODUCT

Cytotec 200 mcg tablets.

 

2. QUALITATIVE AND QUANTITATIVE COMPOSITION

Each tablet contains 200 micrograms misoprostol.

For the full list of excipients, see section 6.1.

 

3. PHARMACEUTICAL FORM

White to off-white hexagonal tablets scored both sides, engraved SEARLE 1461 on one side for oral administration.

 

4. CLINICAL PARTICULARS

4.1 Therapeutic indications

Cytotec is indicated for the healing of duodenal ulcer and gastric ulcer including those induced by nonsteroidal anti-inflammatory drugs (NSAID) in arthritic patients at risk, whilst continuing their NSAID therapy. In addition, Cytotec can be used for the prophylaxis of NSAID-induced ulcers.

 

4.2 Posology and method of administration

Adults

Healing of duodenal ulcer, gastric ulcer and NSAID-induced peptic ulcer: 800 micrograms daily in two or four divided doses taken with breakfast and/or each main meal and at bedtime.

Treatment should be given initially for at least 4 weeks even if symptomatic relief has been achieved sooner. In most patients ulcers will be healed in 4 weeks but treatment may be continued for up to 8 weeks if required. If the ulcer relapses further treatment courses may be given.

Prophylaxis of NSAID-induced peptic ulcer: 200 micrograms twice daily, three times daily or four times daily. Treatment can be continued as required. Dosage should be individualised according to the clinical condition of each patient.

Elderly

The usual dosage may be used.

Renal Impairment: Available evidence indicates that no adjustment of dosage is necessary in patients with renal impairment.

Hepatic Impairment: Cytotec is metabolised by fatty acid oxidising systems present in organs throughout the body. Its metabolism and plasma levels are therefore unlikely to be affected markedly in patients with hepatic impairment.

Children

Use of Cytotec in children has not yet been evaluated in the treatment of peptic ulceration or NSAID-induced peptic ulcer disease.

 

4.3 Contraindications

Misoprostol is contraindicated:

• In women who are pregnant, or in whom pregnancy has not been excluded, or who are planning a pregnancy as misoprostol increases uterine tone and contractions in pregnancy which may cause partial or complete expulsion of the products of conception (see Sections 4.4, 4.6 and 4.8). Use in pregnancy has been associated with birth defects.

• In patients with a known hypersensitivity to misoprostol or to any other component of the product, or to other prostaglandins.

 

4.4 Special warnings and precautions for use

Women of childbearing potential should not be started on misoprostol until pregnancy is excluded, and should be fully counselled on the importance of adequate contraception while undergoing treatment. If pregnancy is suspected, use of the product should be discontinued (see sections 4.3, 4.6 and 4.8).

In such patients it is advised that Cytotec should only be used if the patient:

• takes effective contraceptive measures

• has been advised of the risks of taking Cytotec if pregnant (see section 4.3)

Gastrointestinal bleeding, ulceration, and perforation have occurred in NSAID-treated patients receiving misoprostol. Physicians and patients should remain alert for ulceration, even in the absence of gastrointestinal symptoms, and, where appropriate, endoscopy and biopsy should be carried out before use to ensure that malignant disease is absent in the upper gastrointestinal tract. These investigations and any others considered necessary by the clinician should be repeated at appropriate intervals for follow-up purposes.

Symptomatic responses to misoprostol do not preclude the presence of gastric malignancy.

Misoprostol should be used with caution in patients with conditions that predispose them to diarrhoea, such as inflammatory bowel disease. To minimise the risk of diarrhoea, misoprostol should be taken with food, and magnesium containing antacids should be avoided (see section 4.5).

Misoprostol should be used with caution in patients in whom dehydration would be dangerous. These patients should be monitored carefully.

The results of clinical studies indicate that Cytotec does not produce hypotension at dosages effective in promoting the healing of gastric and duodenal ulcers. Nevertheless, Cytotec should be used with caution in the presence of disease states where hypotension might precipitate severe complications, e.g. cerebrovascular disease, coronary artery disease or severe peripheral vascular disease including hypertension.

There is no evidence that Cytotec has adverse effects on glucose metabolism in human volunteer or patients with diabetes mellitus.

 

4.5 Interaction with other medicinal products and other forms of interaction

Concomitant administration of NSAIDs and misoprostol in rare cases can cause a transaminase increase and peripheral oedema.

Cytotec is predominantly metabolised via fatty acid oxidising systems and has shown no adverse effect on the hepatic microsomal mixed function oxidase (P450) enzyme system. In specific studies no clinically significant pharmacokinetic interaction has been demonstrated with antipyrine or diazepam. A modest increase in propranolol concentrations (mean approximately 20% in AUC, 30% in Cmax) has been observed with multiple dosing of misoprostol. In extensive clinical studies no drug interactions have been attributed to Cytotec. Drug interaction studies with misoprostol and several NSAIDs showed no clinical significant effects on the kinetics of ibuprofen, diclofenac, piroxicam, aspirin, naproxen or indomethacin.

Magnesium-containing antacids should be avoided during treatment with misoprostol as this may worsen the misoprostol-induced diarrhoea.

 

4.6 Fertility, pregnancy and lactation

Pregnancy

Misoprostol is contraindicated in women who are pregnant because it induces uterine contractions and is associated with abortion, premature birth, foetal death and birth defects. First trimester exposure to misoprostol is associated with a significantly increased risk of two birth defects: Mobius sequence (i.e. palsies of cranial nerves VI and VII) and terminal transverse limb defects. Other defects including arthrogryposis have been observed.

The risk of uterine rupture increases with advancing gestational age and with prior uterine surgery, including Caesarean delivery. Grand multiparity also appears to be a risk factor for uterine rupture.

Lactation

Misoprostol is rapidly metabolised in the mother to misoprostol acid, which is biologically active and is excreted in breast milk. Misoprostol should not be administered to nursing mothers because the excretion of misoprostol acid could cause undesirable effects such as diarrhoea in nursing infants.

 

4.7 Effects on ability to drive and use machines

Cytotec can cause dizziness. Patients should be cautioned about operating machinery and driving.

 

4.8 Undesirable effects

The Adverse reaction terms were then categorized utilizing the incidence rate as follows:

Very Common: ≥1/10 (≥10%)

Common: ≥1/100 and <1/10, (≥1% and <10%)

Uncommon: ≥1/1000 and <1/100, (≥0.1% and <1%)

Rare: ≥1/10,000 and <1/1000, (≥0.01% and <0.1%)

Very Rare: <1/10,000, (<0.01%)

Not Known

Immune System Disorder Not Known Anaphylactic reaction
Nervous System Disorders Common Dizziness, headache
Gastrointestinal Disorders
Very common
Common
Diarrhoea*
Abdominal pain*
constipation, dysepsia, flatulence, nausea, vomiting
Skin and Subcutaneous
Tissue Disorders
Very Common
Rash
Pregnancy, puerperium, and perinatal conditions
Not Known
Amniotic fluid embolism, abnormal uterine
contractions, foetal death, incomplete abortion, premature birth, retained placenta, uterine rupture, uterine perforation
Reproductive System and Breast Disorders
Uncommon
 

Rare
Not Known

Vaginal haemorrhage (including postmenopausal bleeding), intermenstrual bleeding, menstrual disorder, uterine cramping
Menorrhagia,
dysmenorrhoea
Uterine haemorrhage
Congenital, Familial and
Genetic Disorders
Not Known
Birth defects
General Disorders and
Administration Site
Conditions
Not Known
Uncommon
 

Chills
Pyrexia

* Diarrhoea and abdominal pain were dose-related, usually developed early in the course of therapy, and were typically self-limiting. Rare instances of profound diarrhoea leading to severe dehydration has been reported.

Diarrhoea can be minimised by using single doses not exceeding 200 micrograms with food and by avoiding the use of predominantly magnesium containing antacids when an antacid is required.

The pattern of adverse events associated with Cytotec is similar when an NSAID is given concomitantly.

Clinical Trials

In clinical trials, over 15,000 patients and subjects received at least one dose of misoprostol. Adverse reactions involved primarily the gastrointestinal system.

Diarrhoea and abdominal pain were dose-related, usually developed early in the course of therapy, and were typically self-limiting. Rare instances of profound diarrhoea leading to severe dehydration have been reported.

The profile for adverse reactions with >1 % incidence was similar for subacute (four to twelve weeks duration) and long-term (up to one year) clinical trials.

The safety of long-term (greater than 12 weeks) administration of misoprostol has been demonstrated in several studies in which patients were treated continuously for up to one year. This includes no adverse or unusual change in the morphology of gastric mucosa, as determined by gastric biopsy.

Special Populations

There were no significant differences in the profile of misoprostol in patients who were 65 years of age or older, compared with younger patients.
The use of misoprostol in children has not been evaluated.

 

4.9 Overdose

Signs and Symptoms of Overdose

The toxic dose of misoprostol in humans has not been determined. Clinical signs that may indicate an overdose are sedation, tremor, convulsions, dyspnea, abdominal pain, diorrhoea, fever, palpitations, hypotension, or bradycardia.

Treatment of Overdose

Because misoprostol is metabolized like a fatty acid, it is unlikely that dialysis would be appropriate treatment for overdosage. In cases of overdose, standard supportive measures should be adopted as required.
In clinical trials patients have tolerated 1200 micrograms daily for three months without significant adverse effects.

 

5 PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Cytotec is an analogue of naturally occurring prostaglandin E1 which promotes peptic ulcer healing and symptomatic relief.

Cytotec protects the gastroduodenal mucosa by inhibiting basal, stimulated and nocturnal acid secretion and by reducing the volume of gastric secretions, the proteolytic activity of the gastric fluid, and increasing bicarbonate and mucus secretion.

 

5.2 Pharmacokinetic properties

Cytotec is rapidly absorbed following oral administration, with peak plasma levels of the active metabolite (misoprostol acid) occurring after about 30 minutes. The plasma elimination half-life of misoprostol acid is 20-40 minutes. No accumulation of misoprostol acid in plasma occurs after repeated dosing of 400 micrograms twice daily.

 

5.3 Preclinical safety data

In single and repeated-dose studies in dogs, rat and mice at multiples of the human dose, toxicological findings were consistent with the known pharmacological effects of the E-type prostaglandins, the main symptoms being diarrhoea, vomiting, mydriasis, tremors and hyperpyrexia. Gastric mucosal hyperplasia was also observed in the mouse, rat and the dog. In the rat and the dog the hyperplasia was reversible on discontinuation of misoprostol following one year of dosing. Histological examination of gastric biopsies in humans has shown no adverse tissue response after up to one year’s treatment. In studies of fertility, teratogenicity and peri/post-natal toxicity in rats and rabbits there were no major findings. A decrease in implantations and some pup growth retardation was observed at doses greater than 100 times the human dose. It was concluded that misoprostol does not significantly affect fertility, is not teratogenic or embryotoxic and does not affect rat pups in the peri/post-natal period.

Misoprostol was negative in a battery of 6 in vitro assays and one in vivo test to assess mutagenic potential. In carcinogenicity studies in the rat and mouse it was concluded that there was no risk of carcinogenic hazard.

 

6. PHARMACEUTICAL PARTICULARS

6.1 List of excipients

Microcrystalline cellulose,
Sodium starch glycolate (Type A),
Hydrogenated castor oil,
Hypromellose.

 

6.2 Incompatibilities

Not applicable.

 

6.3 Shelf life

Keep out of the sight and reach of children.

Do not use Cytotec after the expiry date which is stated on the carton/label after EXP: The expiry date refers to the last day of that month.

 

6.4 Special precautions for storage

Do not store above 30°C. Store in the original package.

 

6.5 Nature and contents of container

Cold-formed aluminium blister packs of 56, 60, 112, 120 or 140 tablets.

Not all pack sizes may be marketed.

 

6.6 Special precautions for disposal and other handling

No Special Requirements.

 

7. FURTHER INFORMATION

MARKETING AUTHORISATION HOLDER

Pharmacia Limited

Ramsgate Road

Sandwich, Kent

CT13 9NJ

United Kingdom

 

MANUFACTURED BY

Piramal Healthcare UK Limited

Morpeth, Whalton Road

Northumberland, NE61 3YA

United Kingdom

 

8. PRESCRIPTION STATUS

Prescription Only Medicine (POM)

 

9. DATE OF REVISION OF THE TEXT

28 November 2013