ENDOCRINE PHARM REVIEW Flashcards by Timothy Carll

Desmopressin

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

Desmopressin

Central Diabetes Insipidus. Also used diagnostically

Recombinant AVP; stimulates V₂R

Can be given IV/SC/PO, usually twice daily

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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.

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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.

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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.

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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.

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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.

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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.

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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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Amiloride & Triamterene

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

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Amiloride & Triamterene

Liddle’s syndrome

Blocks the ENaC channel (downstream of spirono/eplerenone)

Phenoxybenzamine

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

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Phenoxybenzamine

Pheochromocytoma, notably pre-operatively.

Irreversibly blocks alpha receptors.

Orthostatic hypotension (a good goal for pre-op)

Calcitonin

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

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Calcitonin

Treatment of hypercalcemia, osteomalacia, Paget’s disease…(last resort)

Reduce osteoclast activity (weak!)

Tachyphylaxis.

Bisphosphonates

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

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Bisphosphonates

Treatment of hypercalcemia, osteoporosis, osteomalacia, Paget’s…

Induce osteoclast apoptosis by blocking farnesyl synthesis

Esophageal irritation (oral), acute phase reaction, femoral fractures, jaw osteonecrosis.

Ibandronate & Aledronate are oral, Pamedronate and Zanidronic acid are IV (more potent)

Cinacalcet

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

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Cinacalcet

Treatment of hypercalcemia, hyperparathyroidism

Calcimimetic which downregulates PTH production.

Calcium Gluconate

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

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Calcium Gluconate

Acute hypocalcemia.

Just replacement calcium…

Given IV.

**Denosumab** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Denosumab** Osteomalacia & Paget's disease Monoclonal antibody that targets RANK-L to reduce osteoclast differentation. Nausea, fatigue, increased risk of skin infections. -

**Raloxifene** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Raloxifene** Prevention of fractures in osteoporotic patients. Maybe breast cancer. SERM Some increased thrombotic risk -

**Teriparatide** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Teriparatide** Bone anabolism (eg Osteomalacia, osteoporosis) PTH analog, promotes osteoblasts if given intermittently. Transient hypercalcemia, hypercalciuria Given constantly, will stimulate osteoclasts instead.

**Levothyroxine** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Levothyroxine** Hypothyroidism Replacement T₄. Chemically identical to endogenous product! No reported side effects. Give once a day, but half life is about a week.

**Liothyronine** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Liothyronine** Hypothyroidism; more acute than levothyroxine (eg Myxedema coma?) Replacement T₃, chemically indistinguishable. - Shorter lasting than T4, needs more frequent dosing.

**Methimazole** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Methimazole** Hyperthyroidism. Inhibits iodide oxidation. Some lupus-like symptoms, and reversible agranulocytosis. -

**Propylthiouracil** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Propylthiouracil** Hyperthyroidism in early pregnancy. Blocks iodine oxidation, as well as peripheral deiodination to T3. Lupus-like symptoms, reversible agranulocytosis, hepatic failure. -

**Iodide** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Iodide** Hyperthyroidism, pre-op for thyroidectomy, and for radioactive fallout treatment. Reduces thyroid iodine uptake (Wolf-Chaikoff effect). Shrinks and reduces vascularity of thyroid. Acute sensitivity (angioedema, laryngeal edema, serum sickness), head cold.

**¹³¹I** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**¹³¹I** Thyroid ablation (not medullary carcinomas!) Deposits in colloid, produces beta/gamma radiation. Hypothyroidism (lol) -

**Cholestyramine** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Cholestyramine** Hyperthyroidisim Binds and removes thyroid hormone from enterohepatic circulation. - -

**Beta-blockers** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Beta-blockers** Mild hyperthyroidism, pre-op pheochromocytoma Block adrenergic effects of thyroid/pheochromocytoma - -

**Exogenous Insulins** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Exogenous Insulins** Type 1 DM, some Type 2 DM. Replaces deficient insulin production. Downregulates gluconeogenesis, glycogenolysis, glucagon, and lipolysis. Hypoglycemia, allergy, lipoatrophy/hypertrophy, weight gain, edema, "cancer & atherosclerosis" Wide range of insulins & regimens to choose from.

**Sulfonylureas** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Sulfonylureas** Type 2 DM. Stimulate potassium ATPase in pancreatic beta cells to depolarize and release more insulin. Hyponatremia, disulfiram-like reactions, usual stuff, hypoglycemia.

**Metformin** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Metformin** Type 2 DM. Sensitizes the liver to insulin (mainly reduces GNG) GI effects, lactic acidosis. Worse with renal insufficiency, old age, CHF, hypoxia, acute illness, drinking & liver disease. -

**Thiazolidinediones** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Thiazolidinediones** Type 2 DM. Sensitize peripheral tissues to insulin by PPAR receptor agonism. Liver toxicity (troglitazone), weight gain, fluid retention (pedal). CVD mortality (rosiglitazone), bladder cancer. -

**GLP-1 Analogs** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**GLP-1 Analogs** Type 2 DM. Incretin; increases insulin secretion, beta cell mass, weight loss. Inhibits glucagon. Mostly GI, headaches, pancreatitis. Long-lasting, given as SQ (eg Exenatide, liraglutide)

**DPP-4 Inhibitors** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**DPP-4 Inhibitors** Type 2 DM. Prolong GLP-1, see incretin effects. Presumably same as GLP-1 analogs; NVD, headaches, pancreatitis. Given ORALLY.

**SGTP-2 Inhibitors** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**SGTP-2 Inhibitors** Type 2 (and 1?) DM. Increase glucose excretion by blocking sodium-linked transporter in proximal tubule. Yeast infections, dehydration. -

**Alpha-glucosidase inhibitors** Indication? Mechanism of action? Side effects & contraindications? Kinetic considerations?

**Alpha-glucosidase inhibitors** Reduction of post-prandial hyperglycemia. Inhibit enteric enzymes to reduce carbohydrate absorption GI symptoms (diarrhea, flatulence, bloating). Unpopular as a result. -

Here's some drugs, give their classes. Pioglitazone Canagliflozin Glyburide Liraglutide Sitagliptin Acarbose Meglitinide

Pioglitazone - Thiazolidinedione. Canagliflozin - SGPT-1 inhibitor. Glyburide - Sulfonylurea. Liraglutide - GLP-1 agonist. Sitagliptin - DPP-4 inhibitor. Acarbose - Alpha-glucosidase inhibitor. Meglitinide - Almost a sulfonylurea.

**Orlistat** Indication? Mechanism of Action? Side effects & contraindications? Kinetic considerations?

**Orlistat** Weight loss in metabolic syndrome Reversibly inhibits gastric and pancreatic lipases to reduce fat absorption. GI complaints, headache, upper respiratory infection. -

ENDOCRINE PHARM REVIEW Flashcards

(45 cards)