ENDOCRINE PHARM REVIEW Flashcards Preview

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Flashcards in ENDOCRINE PHARM REVIEW Deck (45):
1

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

2

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

-

3

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.

4

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.

5

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.

6

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.

7

Octreotide/Lanreotide

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

Octreotide/Lanreotide

Acromegaly.

Somatostatin agonist, decreases GH secretion.

Diarrhea, abdominal cramping, flatulence, cholelithiasis.

-

8

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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9

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.

-

-

10

Mifepristone

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

Mifepristone

Primary Cushing's disease

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

-

-

11

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.

12

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.

13

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...

-

14

Ketoconazole

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

Ketoconazole

Primary Cushing's syndrome

Adrenal steroidogenesis inhibitor

Liver toxicity

-

15

Metyrapone

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

Metyrapone

Primary Cushing's syndrome

Adrenal steroidogenesis inhibitor (11-beta hydroxylase inhibitor)

-

-

16

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.

-

-

 

17

Etomidate

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

Etomidate

Primary Cushing's disease (especially in critically ill)

Adrenal steroidogenesis inhibitor

-

-

18

Spironolactone & Eplerenone

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

Spironolactone & Eplerenone

Primary hyperaldosteronism.

Mineralocorticoid receptor antagonists.

Hyperkalemia...

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19

Amiloride & Triamterene

Indication?

Mechanism of action?

Side effects / contraindications?

Kinetic considerations?

Amiloride & Triamterene

Liddle's syndrome

Blocks the ENaC channel (downstream of spirono/eplerenone)

-

-

20

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)

-

21

Calcitonin

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

Calcitonin

Treatment of hypercalcemia, osteomalacia, Paget's disease...(last resort)

Reduce osteoclast activity (weak!)

-

Tachyphylaxis.

22

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)

23

Cinacalcet

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

Cinacalcet

Treatment of hypercalcemia, hyperparathyroidism

Calcimimetic which downregulates PTH production.

-

-

24

Calcium Gluconate

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

Calcium Gluconate

Acute hypocalcemia.

Just replacement calcium...

-

Given IV.

25

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.

-

26

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

-

27

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.

28

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.

29

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.

30

Methimazole

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

Methimazole

Hyperthyroidism.

Inhibits iodide oxidation.

Some lupus-like symptoms, and reversible agranulocytosis.

-

31

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.

-

32

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.

33

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)

-

34

Cholestyramine

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

Cholestyramine

Hyperthyroidisim

Binds and removes thyroid hormone from enterohepatic circulation.

-

-

35

Beta-blockers

Indication?

Mechanism of action?

Side effects & contraindications?

Kinetic considerations?

Beta-blockers

Mild hyperthyroidism, pre-op pheochromocytoma

Block adrenergic effects of thyroid/pheochromocytoma

-

-

36

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.

37

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.

38

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.

-

39

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.

40

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)

41

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.

42

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.

-

43

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.

-

44

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.

45

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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