Suplac

Bromocriptine mesylate.

Round, flat, white tablet, bisected on one face and impressed "BIOLAB" on the obverse.
Each tablet contains Bromocriptine mesylate equivalent to Bromocriptine 2.5 mg.

Pharmacology: Pharmacodynamics: Bromocriptine mesylate is an ergot-derivative dopamine receptor agonist and prolactin inhibitor. Bromocriptine reduces serum prolactin concentrations by inhibiting release of prolactin from the anterior pituitary gland by a direct effect on the pituitary and/or by stimulating postsynaptic dopamine receptors in hypothalamus to release prolactin inhibitory factor via a complicated catecholamine pathway.
Pharmacokinetics: Absorption: Bromocriptine is rapidly absorbed from the gastrointestinal tract and peak plasma concentrations occur within 1 to 3 hours after oral doses. However, only about 30% of an oral dose is absorbed and, owing to extensive first-pass metabolism, the bioavailability is only about 6%.
Distribution: Bromocriptine and its metabolites do not distribute appreciably into erythrocytes. In vitro studies have found that bromocriptine is 90-96% bound to serum albumin.
Metabolism: Bromocriptine is extensively metabolized in the gastrointestinal tract and liver, principally by cytochrome P-450 (CYP) 3A4. The metabolites apparently are not pharmacologically active or toxic.
Excretion: Bromocriptine and its metabolites are excreted principally in feces via billiary elimination; approximately 2.5-5.5% of a single dose is excreted in urine. Within 5 days, about 85% of a dose is excreted in feces.

Adults and Pediatrics (aged 7-17 years): The safety and effectiveness of bromocriptine in pediatric patients has only been established for the Prolactinomas and Acromegaly indications, in pediatrics aged 7-17 years.
Prolactinomas: Conservative treatment of prolactin-secreting pituitary micro- or macro-adenomas; Prior to surgery in order to reduce tumour size and to facilitate removal; After surgery if prolactin level is still elevated.
Acromegaly: As an adjunct, or in special cases as an alternative, to surgery or radiotherapy.
Adults: Parkinson's disease: All stages of idiopathic and postencephalitic Parkinson's disease, either as monotherapy or in combination with other antiparkinsonian drugs.
Hyperprolactinaemia in men: Prolactin-related hypogonadism: Anovulatory cycles (supplementary to anti-estrogen, e.g. clomiphene).

Recommended Dose: SUPLAC should always be taken with food.
Adults: Parkinson's disease: In order to ensure optimal tolerability, treatment should be started with a low dose of 1.25 mg (½ tablet) per day, given preferably in the evening. For the first week, SUPLAC should be titrated slowly in order to arrive at the minimal effective dose for each patient. The daily dosage should be increased gradually by 1.25 mg/day each week, and given as 2 to 3 divided doses. An adequate therapeutic response may be reached within 6 to 8 weeks; if it is not, the daily dose may be further increased by 2.5 mg/day each week.
The usual therapeutic range for monotherapy or combined therapy is 10-40 mg bromocriptine per day, but higher doses may be required in some patients.
Should undesirable reactions occur during the titration phase, the daily dose should be reduced and maintained at the lower level for at least a week. If the adverse reactions disappear, the dose can be increased again.
For patients exhibiting motor disorders on levodopa therapy, it is suggested that the levodopa dosage should be reduced before SUPLAC treatment is initiated. When a satisfactory response to SUPLAC has been obtained, a further stepwise reduction in levodopa dosage can be made. In certain patients, levodopa may be withdrawn completely.
Prolactinomas: 1.25 mg (½ tablet) 2 or 3 times daily, gradually increasing to several tablets daily as required to keep plasma prolactin adequately suppressed.
Acromegaly: Initially 1.25 mg (½ tablet) 2 or 3 times daily, gradually increasing to 10 to 20 mg daily, depending on clinical response and side effects.
Hyperprolactinaemia in men: 1.25 mg (½ tablet) 2 or 3 times daily, gradually increasing to 5 to 10 mg per day.
Pediatrics (aged 7-17 years): Prolactinomas: Pediatric population older than 7 years: 1.25 mg (½ tablet) 2 or 3 times daily, gradually increasing to several tablets daily as required to keep plasma prolactin adequately suppressed. Maximum daily dose recommended in children in children aged 7 to 12 tears is 5 mg. Maximum daily dose recommended in adolescent patients (13-17 years) is 20 mg.
Acromegaly: Pediatric population older than 7 years: Initially 1.25 mg (½ tablet) 2 or 3 times daily, gradually increasing to several tablets daily, depending on clinical response and side effects. Maximum daily dose recommended in children aged 7 to 12 years is 10 mg. Maximum daily dose recommended in adolescent patients (13-17 years) is 20 mg.
Special populations: Geriatrics (aged 65 years and above): Even though no variation in efficacy or adverse reaction profile in elderly patients taking SUPLAC has been observed, greater sensitivity in some elderly individuals cannot be ruled out. In general, dose selective for an elderly patient should be cautious, starting at the lower end of the dose range, reflecting the greater frequency of decrease hepatic, renal or cardiac function, and of concomitant disease or other drug therapy in this population.
Renal impairment: No studies have been performed in renally impaired patients.
Hepatic impairment: No studies have been performed in hepatically impaired patients.
Mode of Administration: SUPLAC is administered orally with food.

Symptoms and signs: Overdosage of bromocriptine may cause nausea, vomiting, and severe hypotension.
Treatment: Treatment of bromocriptine overdosage consists of emptying the stomach by aspiration and lavage and administration of IV fluids to treat hypotension.

Hypersensitivity to bromocriptine, ergot alkaloids, or any component of the formulation, and in those with uncontrolled hypertension.
Bromocriptine is contraindicated in the toxaemia of pregnancy.
Bromocriptine is contraindicated in patients with pre-existing valve problems.

Patients with hyperprolactinaemia should be investigated for the possibility of pituitary tumour before treatment with bromocriptine.
Hypotensive reactions may be disturbing in some patients during the first few days of treatment and those who drive or operate machinery should be warned of the possibility of dizziness and fainting during this period.
Treatment of women with hyperprolactinaemic amenorrhoea results in ovulation; patients not wishing to conceive should be advised to use contraceptive measures although oral contraceptives should be avoided.
Bromocriptine should also not be used postpartum or in the puerperium in women with hypertension, coronary artery disease, or symptoms or a history of serious psychiatric disorders. When used, blood pressure should be monitored carefully, especially during the first few days in postpartum women.
Patients on long-term, high dose therapy should be monitored for signs of progressive fibrotic disorders such as retroperitoneal fibrosis.

Pregnancy: Women who have taken bromocriptine during pregnancy indicate that the incidence of spontaneous abortions and congenital malformations appears to be similar to reported in general population. However, dopamine agonists generally should not be used during pregnancy and should be discontinued immediately if pregnancy occurs.
Lactation: Bromocriptine interferes with lactation, the drug should not be used in nursing women.

Nervous system: Headache, migraine, dizziness, drowsiness, fatigue, insomnia, lightheadedness, faintness, fainting, sedation.
Gastrointestinal: Nausea, vomiting, anorexia, abdominal cramps, epigastric pain, dyspepsia, constipation, diarrhea, dry mouth.
Cardiovascular: Postural hypotension, syncope, severe prolonged hypotension, shock, angina, palpitation, arrhythmia, ventricular tachycardia, bradycardia, edema, cold-induced vasospasm with pallor of fingers and toes, exacerbation of Raynaud's syndrome.
Respiratory: Nasal congestion, pulmonary infiltrates, pleural effusion.
Neuromuscular & skeletal: Leg cramps, muscle cramps.
Dermatologic: Rash, mottling skin, facial pallor, urticaria, hair loss.
Optic: Blurred vision, diplopia.

Alcohol (Ethyl): Alcohol (Ethyl) may enhance the adverse/toxic effect of bromocriptine. Bromocriptine may enhance the adverse/toxic effect of Alcohol (Ethyl).
Alpha-/Beta-agonists: Bromocriptine may enhance the hypertensive effect and vasoconstricting effect of Alpha-/Beta-Agonists.
Anti-Parkinson's agents (MAO inhibitors): Anti-Parkinson's agents (MAO inhibitors) may enhance the serotonergic effect. This could result in serotonin syndrome.
Bupropion: Bromocriptine may enhance the adverse/toxic of bupropion.
CYP3A4 Inhibitors: Increased the serum concentration of bromocriptine.
Metoclopramide: Metoclopramide may diminish the effects of bromocriptine.
Antipsychotic agents: Antipsychotic agents may diminish the effects of bromocriptine.
Beta-Blockers: Beta-Blockers may enhance the vasoconstricting effect of bromocriptine.
Macrolides: Increased the serum concentration of bromocriptine.
Barbiturates: Barbiturates may enhance the hypotensive effect of blood pressure lowering.
Levodopa: Bromocriptine may enhance the hypotensive effect of levodopa.

Store at temperature not exceeding 30°C.

Trophic Hormones & Related Synthetic Drugs

G02CB01 - bromocriptine ; Belongs to the class of prolactine inhibitors. Used to suppress lactation.

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