Danazol + Clomiphene Flashcards

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Questions and Answers

What is the name of the drug that is a weak progestin and a weak androgen (partial agonist)?

hMG

Danazol (correct)

Clomiphene

GnRH agonist

What is the mechanism of action (MOA) of Danazol?

Acts directly on the ovary to prevent synthesis of estrogen and progestin by inhibiting certain CYP450s.

How does Danazol act as a partial agonist for androgen receptors?

It has the ability of translocating the androgen receptor to the nucleus causing a response.

What conditions is Danazol used to treat?

Fibrocystic breast condition and endometriosis. Signup and view all the answers

How does Danazol work on treating fibrocystic breast condition?

It prevents synthesis of estrogen. Signup and view all the answers

Although Danazol is used to treat endometriosis, what has replaced Danazol?

GnRH agonist (continuous mode of administration). Signup and view all the answers

What are some side effects when using Danazol?

Reduction in breast size, thickening of skin and increased oiliness, hair growth, deepening of voice (irreversible). Signup and view all the answers

What is Clomiphene citrate?

An estrogen antagonist that acts at hypothalamic and pituitary estrogen receptors. Signup and view all the answers

Clomiphene citrate is used as a fertility agent.

True Signup and view all the answers

What are some adverse effects of Clomiphene citrate?

Hot flashes, breast tenderness, and heavy menses. Signup and view all the answers

When using Clomiphene citrate, what causes hot flashes?

Due to the hypothalamic block. Signup and view all the answers

What causes breast tenderness and heavy menses when using Clomiphene citrate?

Due to too much estrogen later in the cycle. Signup and view all the answers

What is a caution when taking Clomiphene citrate?

Visual symptoms such as blurred vision, floaters, light sensitivity, schotoma. Signup and view all the answers

When Clomiphene citrate is combined with metformin or glitazones, it will enhance fertility of women with polycystic ovary syndrome (PCOS).

True Signup and view all the answers

When do we administer Clomiphene citrate?

Begins at or near the 5th day of the menstrual cycle and is continued for 5 days. Signup and view all the answers

What are the two therapeutic agents that act by altering hormone control mechanisms?

Danazol and Clomiphene citrate. Signup and view all the answers

What must be given after giving a patient Clomiphene citrate?

hCG which mimics LH and causes the LH surge. Signup and view all the answers

If Clomiphene citrate does not work, what other regimen can we use?

hMG for its LH/FSH activity or recombinant FSH + hMG. Signup and view all the answers

Is Clomiphene citrate a SERM?

False Signup and view all the answers

Study Notes

Danazol

Weak progestin and weak androgen (partial agonist) used primarily for treating fibrocystic breast condition and endometriosis.
Mechanism of action involves inhibition of estrogen and progestin synthesis by targeting certain CYP450 enzymes in the ovary.
Acts as a partial agonist for androgen receptors by translocating the receptor to the nucleus to elicit a biological response.
Side effects include reduction in breast size, skin thickening, increased oiliness, hair growth, and irreversible deepening of the voice.
Has largely been replaced by GnRH agonists for endometriosis treatment due to improved options.

Clomiphene Citrate

Functions as an estrogen antagonist at hypothalamic and pituitary estrogen receptors, enhancing release of GnRH, FSH, and LH, thereby increasing chances of ovulation.
Used as a fertility agent, contributing to approximately 10% of multiple births.
Common adverse effects include hot flashes, breast tenderness, and heavy menstrual bleeding.
Hot flashes arise due to hypothalamic block; breast tenderness and heavy menses result from elevated estrogen levels later in the menstrual cycle.
Visual symptoms to monitor include blurred vision, floaters, light sensitivity, and schotoma.
Effective when combined with metformin or glitazones in women with polycystic ovary syndrome (PCOS).
Administered starting around the 5th day of the menstrual cycle for a duration of 5 days.
Requires administration of hCG to mimic LH and induce the LH surge post-clomiphene treatment.
If ineffective, alternatives include human menopausal gonadotropin (hMG) or recombinant FSH plus hMG.
Classified as a selective estrogen receptor modulator (SERM).

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Description

Test your knowledge on Danazol and its mechanisms of action with these flashcards. Learn about its role as a weak progestin and androgen, as well as its effects on estrogen synthesis. Ideal for students studying reproductive pharmacology.