Giga

Each mL contains Megestrol Acetate 40 mg.
Excipients/Inactive Ingredients: Polyoxyl 35 Castor Oil, Polysorbate 80, Glycerin, Sorbitol (Liquid) 70%, Saccharin Sodium, Sodium Benzoate, Anhydrous Citric Acid, Colloidal Silicon Dioxide, Simethicone, Banana Essence, Purified Water.

PHARMACOLOGY: PHARMACODYNAMICS: The major effect experienced by patients while taking megestrol acetate, particularly at high doses, is weight gain, which is usually not associated with water retention, but which is secondary to an increased appetite/food intake and an increase in fat and body cell mass.
It is this effect which forms the basis for use of megestrol acetate in patients with anorexia or weight loss. The mechanism by which megestrol acetate produces its effects in anorexia and cachexia are unclear.
PHARMACOKINETICS: Estimates of plasma levels of megestrol acetate are dependent on the measurement method used. Plasma levels depend on intestinal and hepatic inactivation of the drug, which may be affected by intestinal tract motility, intestinal bacteria, concomitant antibiotic administration, body weight, diet and hepatic function. Metabolites have accounted for only 5% to 8% of an administered dose of megestrol acetate. The major route of drug elimination in humans is urinary excretion averaging approximately 66% and faecal excretion averaging approximately 20% of the administered dose. Respiratory excretion and fat storage may account for the fraction of an administered dose not found in urine or faeces. There are no alterations in pharmacokinetic parameters when megestrol acetate is administered with zidovudine or rifabutin.
Toxicology: PRECLINICAL SAFETY DATA: The chronic administration of megestrol acetate to female dogs for up to 7 years was associated with an increased incidence of both benign and malignant tumours of the breast. Comparable studies in rats and studies in monkeys were not associated with an increased incidence of tumours. The relationship of chronic megestrol acetate exposures and associated dog tumours to cancer induction in humans is unknown, but should be considered in assessing the benefit-to-risk ratio when prescribing Giga, and in surveillance of patients on therapy Fertility and reproduction studies with high doses of megestrol acetate have shown a reversible feminising effect on some male rat foetuses.

Giga Oral Suspension 40 mg/mL is indicated in male and female patients for the treatment of anorexia or weight loss secondary to cancer or AIDS.

Posology: Adults: 400-800 mg given as a single daily dose.
At least two months of continuous treatment is considered an adequate period for determining the efficacy of Giga Oral Suspension.
Paediatric population: The safety and efficacy of Giga Oral Suspension in children have not been established. This medicine is not recommended for use in children.
Elderly: In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy (see Precautions).
Renal impairment: Megestrol acetate is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function.
Method of administration: For oral use only. Shake well immediately before dosing.
A plastic dosage cup with markings is provided for convenience.

No acute toxicological effects have resulted from studies involving megestrol acetate administered in dosages as high as 1600 mg/day for six months or more. Reports of overdose have been received in the postmarketing setting. Signs and symptoms reported in the context of overdose included diarrhoea, nausea, abdominal pain, shortness of breath, cough, unsteady gait, listlessness, and chest pain. There is no specific antidote for overdose with Giga. In case of overdose, appropriate supportive measures should be taken.

Giga is contraindicated in patients who have demonstrated hypersensitivity to the active substance or to any of the excipients listed in Description.
Giga is also contraindicated in patients with thromboembolic disorders.

Giga should be used with caution in patients with a history of thrombophlebitis. This product should be used under the supervision of a specialist and the patients kept under regular surveillance (see Adverse Reactions and PHARMACOLOGY: Toxicology: PRECLINICAL SAFETY DATA under Actions). This product can exert adrenocortical effects. This should be borne in mind in patient surveillance (see Adverse Reactions). Other reported clinical experience has not identified differences in responses between elderly and younger patients. In general, dose selection for elderly patients should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. Megestrol acetate is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken during treatment with megestrol acetate, and it may be useful to monitor renal function.
EFFECTS ON ABILITY TO DRIVE AND USE MACHINES: Giga Oral Suspension has no or negligible influence on the ability to drive or use machines.

Pregnancy: Giga is not recommended for women who are pregnant or who are breast feeding. Women of child bearing potential should be advised to avoid becoming pregnant. Several reports suggest an association between intrauterine exposure to progestational drugs in the first trimester of pregnancy and genital abnormalities in male and female foetuses. The risk of hypospadias, 5 to 8 per 1,000 in male births in the general population may be approximately doubled with the exposure to progestational drugs. If a patient is exposed to megestrol acetate during the first four months of pregnancy or if she becomes pregnant whilst taking megestrol acetate, she should be apprised of the potential risks to the foetus.
Breastfeeding: Because of the potential for adverse effects, nursing should be discontinued during treatment with Giga.
Fertility: There are insufficient data to quantify the risk to exposed female foetuses; however some progestational drugs may cause mild virilisation of the external genitalia of the female fetuses.

Pituitary adrenal axis abnormalities including glucose intolerance, new onset diabetes, exacerbation of pre-existing diabetes with decreased glucose tolerance and Cushing's syndrome have been reported with the use of megestrol acetate. Clinically apparent adrenal insufficiency has been rarely reported in patients shortly after discontinuing megestrol acetate. The possibility of adrenal suppression should be considered in all patients taking or withdrawing from chronic megestrol acetate therapy. Replacement stress doses of glucocorticoids may be indicated. Patients should be observed when Giga is abruptly withdrawn. In clinical trials in patients with AIDS there was no significant difference between active and placebo treatment in patients reporting at least one adverse event. Events reported in ≥ 5% of these study patients included diarrhoea, impotence, rash. Other reported adverse events included flatulence, asthenia, and pain. Similarly in patients with advanced non-endocrine sensitive cancer who received megestrol acetate for anorexia and weight loss, dyspnoea, nausea, oedema, pain, lethargy and diarrhea were commonly observed. Constipation and urinary frequency have also been reported in patients who received high doses of megestrol acetate in clinical trials. A rarely encountered side effect of prolonged administration of megestrol acetate is urticaria, presumably an idiosyncratic reaction to the drug.
The drug is devoid of the myelosuppressive activity characteristic of many cytotoxic drugs and it causes no significant changes in haematology, blood chemistry or urinalysis. The list is presented by system organ class, MedDRA preferred term, and frequency using the following frequency categories: very common (≥1/10), common (≥1/100, <1/10), uncommon (≥1/1000, <1/100), rare (≥1/10000, <1/1000), very rare (<1/10000), and not known (cannot be estimated from the available data). (See table.)

Click on icon to see table/diagram/image

No interaction studies have been performed.

INCOMPATIBILITIES: Not applicable.
SPECIAL PRECAUTIONS FOR DISPOSAL OF A USED MEDICINAL PRODUCT OR WASTE MATERIALS DERIVED FROM SUCH MEDICINAL PRODUCT AND OTHER HANDLING OF THE PRODUCT: No special requirements.

After dosing, store Giga below 30°C and dispense in a tight and light resistant container.
SHELF-LIFE: 3 years.

Cancer Hormone Therapy

L02AB01 - megestrol ; Belongs to the class of progestogens.

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