ENDOCRINE PHARM REVIEW Flashcards

1
Q

Desmopressin

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Desmopressin

Central Diabetes Insipidus. Also used diagnostically

Recombinant AVP; stimulates V2R

-

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

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2
Q

Conivaptan/Talvaptan

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Conivaptan/Talvaptan

SIADH management

Blocks V2R to reduce AQ2 translocation.

Rare association with liver failure

-

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3
Q

Demeclocycline

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

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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4
Q

hGH

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

hGH

GH deficiency (eg short stature)

Recombinant growth hormone…

Rare: SCFE, scoliosis, pseudotumor cerebri, apnea

Give each evening, subQ.

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5
Q

Cabergoline

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

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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6
Q

Bromocriptine

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Bromocriptine

Hyperprolactinemia (1st trimester pregnancies)

Dopamine agonist, downregulates prolactin

As cabergoline, but generally worse.

Shorter half-life, requires frequent dosing.

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7
Q

Octreotide/Lanreotide

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Octreotide/Lanreotide

Acromegaly.

Somatostatin agonist, decreases GH secretion.

Diarrhea, abdominal cramping, flatulence, cholelithiasis.

-

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8
Q

Pegvisomant

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Pegvisomant

(refractory) Acromegaly.

GH receptor antagonist (mainly at liver)

Transient liver panel elevation, tumor growth

-

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9
Q

Megestrol Acetate

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Megestrol Acetate

Cachexia of cancer patients

Progesterone compound, suppresses ACTH and cortisol. Stimulates appetite, apparently.

-

-

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10
Q

Mifepristone

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Mifepristone

Primary Cushing’s disease

Glucocorticoid receptor antagonist. (Note: may precipitate adrenal insufficiency)

-

-

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11
Q

Hydrocortisone

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

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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12
Q

Fludrocortisone

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Fludrocortisone

Primary (not secondary!) adrenal insufficiency.

Exogenous mineralocorticoid…

See hyperaldosteronism

Take daily, monitor plasma renin.

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13
Q

Pasireotide

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Pasireotide

Secondary Cushing’s syndrome (refractory to surgery)

Somatostatin analog; reduces ACTH secretion.

Numerous side effects: diarrhea, nausea, hyperglycemia, headache…

-

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14
Q

Ketoconazole

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Ketoconazole

Primary Cushing’s syndrome

Adrenal steroidogenesis inhibitor

Liver toxicity

-

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15
Q

Metyrapone

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Metyrapone

Primary Cushing’s syndrome

Adrenal steroidogenesis inhibitor (11-beta hydroxylase inhibitor)

-

-

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16
Q

Mitotane

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Mitotane

Primary Cushing’s diseease (due to carcinoma)

Adrenal steroidogenesis inhibitor, lytic in high doses.

-

-

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17
Q

Etomidate

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Etomidate

Primary Cushing’s disease (especially in critically ill)

Adrenal steroidogenesis inhibitor

-

-

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18
Q

Spironolactone & Eplerenone

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Spironolactone & Eplerenone

Primary hyperaldosteronism.

Mineralocorticoid receptor antagonists.

Hyperkalemia…

-

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19
Q

Amiloride & Triamterene

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

A

Amiloride & Triamterene

Liddle’s syndrome

Blocks the ENaC channel (downstream of spirono/eplerenone)

-

-

20
Q

Phenoxybenzamine

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Phenoxybenzamine

Pheochromocytoma, notably pre-operatively.

Irreversibly blocks alpha receptors.

Orthostatic hypotension (a good goal for pre-op)

-

21
Q

Calcitonin

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Calcitonin

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

Reduce osteoclast activity (weak!)

-

Tachyphylaxis.

22
Q

Bisphosphonates

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

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)

23
Q

Cinacalcet

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Cinacalcet

Treatment of hypercalcemia, hyperparathyroidism

Calcimimetic which downregulates PTH production.

-

-

24
Q

Calcium Gluconate

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Calcium Gluconate

Acute hypocalcemia.

Just replacement calcium…

-

Given IV.

25
Q

Denosumab

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Denosumab

Osteomalacia & Paget’s disease

Monoclonal antibody that targets RANK-L to reduce osteoclast differentation.

Nausea, fatigue, increased risk of skin infections.

-

26
Q

Raloxifene

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Raloxifene

Prevention of fractures in osteoporotic patients. Maybe breast cancer.

SERM

Some increased thrombotic risk

-

27
Q

Teriparatide

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Teriparatide

Bone anabolism (eg Osteomalacia, osteoporosis)

PTH analog, promotes osteoblasts if given intermittently.

Transient hypercalcemia, hypercalciuria

Given constantly, will stimulate osteoclasts instead.

28
Q

Levothyroxine

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Levothyroxine

Hypothyroidism

Replacement T4. Chemically identical to endogenous product!

No reported side effects.

Give once a day, but half life is about a week.

29
Q

Liothyronine

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Liothyronine

Hypothyroidism; more acute than levothyroxine (eg Myxedema coma?)

Replacement T3, chemically indistinguishable.

-

Shorter lasting than T4, needs more frequent dosing.

30
Q

Methimazole

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Methimazole

Hyperthyroidism.

Inhibits iodide oxidation.

Some lupus-like symptoms, and reversible agranulocytosis.

-

31
Q

Propylthiouracil

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Propylthiouracil

Hyperthyroidism in early pregnancy.

Blocks iodine oxidation, as well as peripheral deiodination to T3.

Lupus-like symptoms, reversible agranulocytosis, hepatic failure.

-

32
Q

Iodide

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

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.

33
Q

131I

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

131I

Thyroid ablation (not medullary carcinomas!)

Deposits in colloid, produces beta/gamma radiation.

Hypothyroidism (lol)

-

34
Q

Cholestyramine

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Cholestyramine

Hyperthyroidisim

Binds and removes thyroid hormone from enterohepatic circulation.

-

-

35
Q

Beta-blockers

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Beta-blockers

Mild hyperthyroidism, pre-op pheochromocytoma

Block adrenergic effects of thyroid/pheochromocytoma

-

-

36
Q

Exogenous Insulins

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

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.

37
Q

Sulfonylureas

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Sulfonylureas

Type 2 DM.

Stimulate potassium ATPase in pancreatic beta cells to depolarize and release more insulin.

Hyponatremia, disulfiram-like reactions, usual stuff, hypoglycemia.

38
Q

Metformin

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

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.

-

39
Q

Thiazolidinediones

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

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.

-

40
Q

GLP-1 Analogs

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

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)

41
Q

DPP-4 Inhibitors

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

DPP-4 Inhibitors

Type 2 DM.

Prolong GLP-1, see incretin effects.

Presumably same as GLP-1 analogs; NVD, headaches, pancreatitis.

Given ORALLY.

42
Q

SGTP-2 Inhibitors

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

SGTP-2 Inhibitors

Type 2 (and 1?) DM.

Increase glucose excretion by blocking sodium-linked transporter in proximal tubule.

Yeast infections, dehydration.

-

43
Q

Alpha-glucosidase inhibitors

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

A

Alpha-glucosidase inhibitors

Reduction of post-prandial hyperglycemia.

Inhibit enteric enzymes to reduce carbohydrate absorption

GI symptoms (diarrhea, flatulence, bloating). Unpopular as a result.

-

44
Q

Here’s some drugs, give their classes.

Pioglitazone

Canagliflozin

Glyburide

Liraglutide

Sitagliptin

Acarbose

Meglitinide

A

Pioglitazone - Thiazolidinedione.

Canagliflozin - SGPT-1 inhibitor.

Glyburide - Sulfonylurea.

Liraglutide - GLP-1 agonist.

Sitagliptin - DPP-4 inhibitor.

Acarbose - Alpha-glucosidase inhibitor.

Meglitinide - Almost a sulfonylurea.

45
Q

Orlistat

Indication?

Mechanism of Action?

Side effects & contraindications?

Kinetic considerations?

A

Orlistat

Weight loss in metabolic syndrome

Reversibly inhibits gastric and pancreatic lipases to reduce fat absorption.

GI complaints, headache, upper respiratory infection.

-