Drugs Flashcards
(16 cards)
What is clomiphene
Clomiphene is a selective estrogen receptor modulator *SERM), and antagnoizes hyothalamic-pituatary estrogen receptor alpha
ERalpha - promoting fertility
What estrogen receptor alpha does is in the hypothalamus it detects estrogen secreted by the granulosa cells and via negative feedback, ablates FSH secretion and downmodulates LH.
With Clomiphene you are promoting fertility by blocking the negative feedback thereby increasing FSH and leading to the formation of more dominant follicles.
What is Leuprolide
Luprolide is a GnRH agonist
generally reserved for anovulatory women who fail to
respond to other less complicated forms of treatment (e.g., clomiphene).
• They are most commonly used for controlled ovarian hyperstimulation (COH) in
assisted reproductive procedures, such as in vitro fertilization (IVF).
GnRH analog with agonist properties
when used in pulsatile fashion; antagonist
properties when used in continuous fashion
(downregulates GnRH receptor in pituitary
leading to decreased FSH and LH).
Leuprolide can be used in lieu of GnRH.
CLINICAL USE Uterine fibroids, endometriosis, precocious puberty, prostate cancer, infertility.
ADVERSE EFFECTS Hypogonadism, decreased libido, erectile dysfunction, nausea, vomiting.
What are Dexamethasone and; Prednisone
They are glucocorticoid analogues
What is Fludrocortisone
Fludricortisone is a mineralcorticoid agonist (aldosterone
What are Bromocryptine and Cabergoline?
Bromocryptine and Cabergoline are dopamine receptor agonists. Dopamine blocks PRL secretion.
Bromocryptine also can antagonize GH secretion under conditions of pathophysiology. -in a significant amount of pituitary adenomas, prolactin and GH become coupled so inhibit prolactin with dopamine, inhibit GH secretion.
PRL: Prolactin (PRL), also known as luteotropic hormone or luteotropin, is a protein that in humans is best known for its role in enabling mammals, usually females, to produce milk
What are Octreotide and Lanreotide?
Octreotide is a somatostatin analogue; impairs GH secretion
Somatostain: growth hormone inhibiting protein. Somatostatin inhibits insulin and glucagon secretion
What is Pegvisomant?
Pegvisomant is a Growth Hormone Receptor antagonist.
What are tocolytic agents?
They are competitive inhibitors of calcium and aim to keep the myometrium quiet. This is to prevent preterm labor
What is effect of PRL?
PRL is a stress hormone and it knocks out the GnRH pulse generator. This is why lactating also prevents cycling.
What is dexamethasone?
Dexamethasone is a really potent glucocorticoid analogue. As a result, the dexamethasone suppression test for Cushings relies on the negative feedback cortisol has on ACTH. Dex should decrease both ACTH and Cortisol.
A patient with Cushings has a higher threshold for negative feedback and this loss of baseline negative feedback allows the ACTH and cortisol to remain elevated in a low dose dex suppression test.
in HIGH dose, there are two outcomes. ACTH will be lowered in Cushing disease
ACTH will remain elevated because the Cushing syndrome is not neuroendocrine in origin. Could be an ACTH secreting tumor in the adrenal cortex which is therefore not affected by negative feedback.
What are bisphosphonates good for?
They are good replacement after a women undergoes menopause and have decreasing estrogen levels.
Bisphosphonates promote osteoclast apoptosis and decrease osteoclast activity .
How does a oral contraceptive of estrogen and progesterone combination work?
Progestins and ethinyl estradiol; forms include pill, patch, vaginal ring.
Estrogen and progestins inhibit LH/FSH and thus prevent estrogen surge. No estrogen surge > no
LH surge > no ovulation.
Progestins cause thickening of cervical mucus, thereby limiting access of sperm to uterus.
Progestins also inhibit endometrial proliferation
so the endometrium is less suitable to the
implantation of an embryo.
Contraindications: smokers > 35 years old (increases risk of cardiovascular events),
-patients with risk of cardiovascular disease (including
-history of venous thromboembolism, coronary artery disease, stroke),
-migraine (especially with aura),
-breast cancer,
-liver disease.
Progesterone counters cancerous effects of too much estrogen.
Clomiphene
Antagonist at estrogen receptors in hypothalamus. Prevents normal feedback inhibition and
decreases release of LH and FSH from pituitary, which stimulates ovulation.
Used to treat infertility due to anovulation (eg, PCOS). Where there is increased LH to FSH ratio.
SERMs may cause hot flashes, ovarian enlargement, -multiple simultaneous pregnancies, visual disturbances.
Ceftriaxone (repro)
Typically caused by exposure to disease-causing microorganisms like Neisseria
gonorrhoeae and Chlamydia trachomatis.
• The only parenteral antibiotic now recommended by the CDC for the treatment of gonorrhea is ceftriaxone.
• 50% of women and 20% of men with gonorrhea have a co-existing chlamydial
infection.
• For this reason, concomitant oral treatment with azithromycin or doxycycline is
recommended in all patients treated for gonorrhea
Ceftriaxone is a 3rd-generation cephalosporin.
• Cephalosporins are b-lactam antibiotics that inhibit the biosynthesis of the
bacterial cell wall.
• This activity results in bacterial cell death (it is bactericidal)
Azithromycin (50S) is a macrolide antibiotic and doxycycline (30S) is a tetracycline analog.
• Both are long-acting, orally bioavailable agents.
• Both agents inhibit bacterial protein synthesis resulting in the inhibition of bacterial
growth (they are bacteriostatic).
metronidazole (repro)
Trichomonas - Typically caused by exposure to the flagellated protozoan Trichomonas
vaginalis.
• Co-infection with other STDs (e.g., gonorrhea) is not unusual.
• More commonly reported in women than men.
• Infected women typically present with a malodorous vaginal discharge of pH >5.
• A wet-mount examination is most reliable means of diagnosis (look for pearshaped
flagellating organism).
Metronidazole is a nitroimidazole drug that kills
anaerobic bacteria and susceptible protozoans
(including T. vaginalis).
• Activation of the drug requires the enzyme pyruvateferredoxin oxidoreductase (PFOR) found in
susceptible microbes.
• Activation using ferredoxin (Fd) as the electron donor
results in the reduction of the nitro (NO2) group to
form a toxic radical.
• The toxic radical oxidatively damages microbial DNA
leading to fragmentation and cell death.
Taking the drug with meals lessens GI irritation
Nausea and vomiting is enhanced if with ingestion of alcohol.
• Use with caution in patients with CNS disease.
• Contraindicated in the first trimester of pregnancy (pregnancy category B).
• Secreted in breast milk. Nursing mothers should cease breast feeding for 12-24
hours after ingestion of the drug
acyclovir, valacyclovir, and famciclovir (repro)
commonly used for (HSV-2).
Acyclovir and penciclovir are acyclic guanosine
analogs that require a viral kinase to be activated.
• The drugs are therefore selectively activated in
infected cells.
• They inhibit viral DNA synthesis in two ways:
1. Competitive inhibition of viral DNA
polymerase
2. Chain termination after incorporation
into viral DNA
Resulting in Reduced viral shedding
Shorter duration of symptoms
Reduced time for ulcers to heal
