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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Amiloride & Triamterene
Indication?
Mechanism of action?
Side effects / contraindications?
Kinetic considerations?
Amiloride & Triamterene
Liddle’s syndrome
Blocks the ENaC channel (downstream of spirono/eplerenone)
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Phenoxybenzamine
Indication?
Mechanism of action?
Side effects & contraindications?
Kinetic considerations?
Phenoxybenzamine
Pheochromocytoma, notably pre-operatively.
Irreversibly blocks alpha receptors.
Orthostatic hypotension (a good goal for pre-op)
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Calcitonin
Indication?
Mechanism of action?
Side effects & contraindications?
Kinetic considerations?
Calcitonin
Treatment of hypercalcemia, osteomalacia, Paget’s disease…(last resort)
Reduce osteoclast activity (weak!)
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Tachyphylaxis.
Bisphosphonates
Indication?
Mechanism of action?
Side effects & contraindications?
Kinetic considerations?
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?
Cinacalcet
Treatment of hypercalcemia, hyperparathyroidism
Calcimimetic which downregulates PTH production.
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Calcium Gluconate
Indication?
Mechanism of action?
Side effects & contraindications?
Kinetic considerations?
Calcium Gluconate
Acute hypocalcemia.
Just replacement calcium…
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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.
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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
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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.
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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.
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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.
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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)
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Cholestyramine
Indication?
Mechanism of action?
Side effects & contraindications?
Kinetic considerations?
Cholestyramine
Hyperthyroidisim
Binds and removes thyroid hormone from enterohepatic circulation.
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Beta-blockers
Indication?
Mechanism of action?
Side effects & contraindications?
Kinetic considerations?
Beta-blockers
Mild hyperthyroidism, pre-op pheochromocytoma
Block adrenergic effects of thyroid/pheochromocytoma
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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.
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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.
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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.
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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.
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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.
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