ENDOCRINE PHARM REVIEW Flashcards
Desmopressin
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Desmopressin
Central Diabetes Insipidus. Also used diagnostically
Recombinant AVP; stimulates V2R
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Can be given IV/SC/PO, usually twice daily
Conivaptan/Talvaptan
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Conivaptan/Talvaptan
SIADH management
Blocks V2R to reduce AQ2 translocation.
Rare association with liver failure
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Demeclocycline
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Demeclocycline
SIADH management
Inhibits the collecting tubules response to AVP
Nephrotoxic (rarely used)
Takes up to one week to be effective.
hGH
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
hGH
GH deficiency (eg short stature)
Recombinant growth hormone…
Rare: SCFE, scoliosis, pseudotumor cerebri, apnea
Give each evening, subQ.
Cabergoline
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Cabergoline
Hyperprolactinemia. Adjunct for acromegaly, secondary Cushing’s…
Agonizes dopamine receptors, downregulating prolactin
N/V, orthostatic hypotension, rare cardiac valvulopathy in Parkinson’s patients.
Better half life, affinity, (everything) than bromocriptine.
Bromocriptine
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Bromocriptine
Hyperprolactinemia (1st trimester pregnancies)
Dopamine agonist, downregulates prolactin
As cabergoline, but generally worse.
Shorter half-life, requires frequent dosing.
Octreotide/Lanreotide
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Octreotide/Lanreotide
Acromegaly.
Somatostatin agonist, decreases GH secretion.
Diarrhea, abdominal cramping, flatulence, cholelithiasis.
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Pegvisomant
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Pegvisomant
(refractory) Acromegaly.
GH receptor antagonist (mainly at liver)
Transient liver panel elevation, tumor growth
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Megestrol Acetate
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Megestrol Acetate
Cachexia of cancer patients
Progesterone compound, suppresses ACTH and cortisol. Stimulates appetite, apparently.
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Mifepristone
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Mifepristone
Primary Cushing’s disease
Glucocorticoid receptor antagonist. (Note: may precipitate adrenal insufficiency)
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Hydrocortisone
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Hydrocortisone
Primary > secondary adrenal insufficiencies.
Exogenous glucocorticoid…
See Cushing’s syndrome.
Can be given orally (daily). Give IM/IV in acute crisis or pre-op.
Fludrocortisone
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Fludrocortisone
Primary (not secondary!) adrenal insufficiency.
Exogenous mineralocorticoid…
See hyperaldosteronism
Take daily, monitor plasma renin.
Pasireotide
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Pasireotide
Secondary Cushing’s syndrome (refractory to surgery)
Somatostatin analog; reduces ACTH secretion.
Numerous side effects: diarrhea, nausea, hyperglycemia, headache…
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Ketoconazole
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Ketoconazole
Primary Cushing’s syndrome
Adrenal steroidogenesis inhibitor
Liver toxicity
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Metyrapone
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Metyrapone
Primary Cushing’s syndrome
Adrenal steroidogenesis inhibitor (11-beta hydroxylase inhibitor)
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Mitotane
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Mitotane
Primary Cushing’s diseease (due to carcinoma)
Adrenal steroidogenesis inhibitor, lytic in high doses.
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Etomidate
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Etomidate
Primary Cushing’s disease (especially in critically ill)
Adrenal steroidogenesis inhibitor
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Spironolactone & Eplerenone
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Spironolactone & Eplerenone
Primary hyperaldosteronism.
Mineralocorticoid receptor antagonists.
Hyperkalemia…
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