Gonablok 200 Capsule

Gonablok 200 mg is a formulation of Danazol i.e., an attenuated androgen and antigonadotropin that acts as a pituitary gonadotropin inhibitor. Used mainly in the condition of endometriosis, fibrocystic breast disease, and hereditary angioedema. It may work by suppressing pituitary gonadotropins, lowering estrogen or progesterone and creating high androgen, low estrogen state.

Key Features

How does Gonablok 200 mg work?

• Suppresses pituitary LH/FSH i.e., by reducing luteinizing hormone and follicle-stimulating hormone mid-cycle surge. 
• Creates hypoestrogenic state just by lowering LH/FSH, as ovaries make less Estradiol. This causes endometrial tissue to become atrophic and inactive.
• It binds to androgen, progesterone, and glucocorticoid receptors. Displaces testosterone from sex hormone-binding globulin that lead to increase in free testosterone. 
• In the case of hereditary angioedema there is increase in C1 esterase inhibitor levels, reducing attacks.
• Direct effect on endometriotic tissue just by inhibiting endometrial cell growth and has anti-inflammatory effects.

Usage

It can be used in treating the following conditions:

• Endometriosis
• Fibrocystic breast disease
• Hereditary angioedema

Dosage

• Dosage may can vary from individual to individual, always take dosage after consulting it from healthcare provider.
• It can be taken with food to reduce GI upset. If you miss a dose, take when remembered unless close to next dose.

Side effects

• Weight gain
• Edema
• Acne
• Oily skin
• Decreased breast size
• Clitoral hypertrophy
• Hair loss
• Hot flushes
• Sweating
• Vaginal dryness/irritation
• Menstrual irregularity
• Amenorrhea

Interaction

• Warfarin: Danazol may increase anticoagulant effect this may increase bleeding risk. Monitor INR closely, reduce warfarin dose.
• Carbamazepine: Danazol inhibits metabolism increase carbamazepine levels/toxicity.
• If the level of Cyclosporine/Tacrolimus gets increase this led to nephrotoxicity.
• Statins increase the risk of myopathy/rhabdomyolysis with simvastatin, lovastatin.
• Insulin/Oral hypoglycaemics as Danazol may cause insulin resistance.
• Danazol can cause fluid retention this may reduce antihypertensive effect.
• Just after lab-tests it is concluded that it may interact with testosterone, androstenedione, DHEA-S assays.

Pharmacokinetics

• Absorption: Oral, variable. Bioavailability increase with food and also reaches the Peak plasma at just 2–8 hours.
• Distribution: Highly lipophilic. Distributes widely. Binds to SHBG, albumin. Vd large.
• Metabolism: Liver extensive first-pass. CYP3A4 major. Main metabolites: ethisterone, 2-hydroxymethyl-danazol.
• Half-life is approx. about 4.5 hours initially, but 26 hours for major metabolite. Effects persist due to pituitary suppression.
• Excretion: Metabolites excreted in urine and feces. Minimal unchanged drug in urine.

Precautions

• Pregnant and breast-feeding women should avoid taking such medications as it may lead to severe side effects.
• The one with prior condition of liver disease, lipid disorder, polycythemia, androgen dependent tumour should avoid taking such medications.

Conclusion

Gonablok 200 mg is a formulation of Danazol i.e. an attenuated androgen and antigonadotropin that acts as a pituitary gonadotropin inhibitor. Used mainly in the condition of endometriosis, fibrocystic breast disease, and hereditary angioedema. It may work by suppressing pituitary gonadotropins, lowering estrogen or progesterone and creating high androgen, low estrogen state. It may have some side effects like weight gain, Edema, acne, oily skin, decreased breast size, clitoral hypertrophy, hair loss, hot flushes, sweating, vaginal dryness/irritation, menstrual irregularity and amenorrhea. This may can vary from person to person so it is needed to consult your doctor or healthcare provider to avoid any such interactions.

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