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Pharmacology Flashcards

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1
Q

What is the use and mechanism of cyclosporine?

A

It is a calcineurin inhibitor that blocks IL2 transcription by binding cyclophilin. It is used as a prophylactic tx of organ rejection, psoriasis and Rheumatoid Arthritis.

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2
Q

What are the major side-effects of cyclosporine?

A

It is nephrotoxis, neurotoxic, causes HTN and hyperlipidemia, hirsutism, and gingival hyperplasia.

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3
Q

What is the use and mechanism of Tacrolimus? Toxicities?

A

It is a calcineurin inhibitor that binds FK506BP, thus inhibiting IL2 transcription. It is used prophylactically to prevent organ rejection. Like cyclosporine, it is neurotoxic and nephrotoxic. It also increases the risk of DM.

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4
Q

What is the use and mechanism of Sirolimus?

A

It is an mTOR inhibitor that binds FKB(like tacrolimus), inhibiting T-cell activation and B-cell differentiation. It is specifically used to prevent kidney transplant rejection. It is preferred for renal transplants because it is NOT Nephrotoxic. However, it can cause pancytopenia, insulin resistance and hyperlipidemia.

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5
Q

What is azothioprine?

A

It is a 6-MP precursor requiring bioactivation. It acts as an antimetabolite of purine synthesis and lymphocyte proliferation. It is used for transplants, RA, Crohn’s Disease and other lymphocyte mediated autoimmune diseases. It causes pancytopenia because it also inhibits myeloid stem cell proliferation..

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6
Q

How do glucocorticoids work?

A

They inhibit NF-kappaBeta from acting as a TF, preventing transcription of cytokines necessary for lymphocyte activation.

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7
Q

Name 3 Rapid-Acting Insulins and their role in DM Tx

A

Aspart, Glulisine, Lispro. They are used for post-prandial glucose control in types 1 and 2 DM

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8
Q

What is the role of recombinant insulin?

A

It is a short acting insulin, used in hospitals via IV for titratable insulin delivery in DKA

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9
Q

List intermediate and long acting insulins and their role

A

Intemrediate=NPH, 2x/day basal insulin

Long acting=Detemir and Glargine, 1x/day, basal insulin

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10
Q

List the mechanism and use of metformin

A

It acts in an unknown mechanism to decrease gluconeogenesis in the liver, increase glycolysis and increase peripheral glucose uptake. It is a FIRST LINE Tx in DM2 that also causes modest weight loss. Its major side-effect is lactic acidosis, and is therefore contraindicated in renal insufficency (difficulty regulating serum pH)

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11
Q

What are the mechanisms and uses of Sulfonylureas?

A

They close K+ channels in beta cells, causing release of stored insulin. Their main toxicities are hypoglycemia (second gen) from excess peripheral glucose uptake.

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12
Q

Name 2 first gen sulfonylureas

A

chlorpropamide, tolbutamide

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13
Q

What are 3 second gen sulfonylureas?

A

glimeperide, glipizide, glyburide, The “GLI/Y”s

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14
Q

What are the Thiazolidinediones?

A

The “GLITAZONES” are DM2 drugs that cause increased insulin sensitivity in the periphery and act by binding PPARgamma. They increase lipid storage and decrease circulating lipids to cause increased glucose utilization. It is a monotherapy for DM2.
Adverse=weight gain from lipid storage; hepatotoxicity from increased hepatic lipid deposition, edema that can exacerbate HF, and fracture increases.

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15
Q

What are exanatide and liraglutide?

A

They are GLP-1 analogs that increase insulin secretion and decrease glucagon release. This causes more immediate pancreas responses to meals which better regulates blood glucose. It also slows stomach emptying to allow prolonged glucose regulation. It is appetite suppressive, aiding in weight loss.

Toxicity is pancreatitis, nausea and vomiting(it is gilla venom DUDE!)

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16
Q

What are the gliptins?

A

They are DPP4 inhibitors, causing increased endogenous GLP1 levels by decreased degradation. Similar use and profile to GLP1 analogs.

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17
Q

What is Pramlintide?

A

amylin analog that slows gastric emptying and lowers glucagon. Last line DM2.

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18
Q

What is Canagliflozin?

A

It is an SGLT2 Inhibitor. It prevents reabsorption of glucose in the proximal tubule of the kidney, resulting in lowered serum glucose. The resulting glucosuria increases susceptibility to UTIs and vaginal yeast infections. SeaGLZ-in

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19
Q

What is the role of acarbose and maglitol in DM management?

A

They are alpha glucosidase inhibitors, preventing disaccharide hydrolysis at brush borders in the intestines and lowered glucose uptake. It reduces post-prandial hyperglycemia.

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20
Q

What are propelthiouracil and methimazole?

A

Both inhibit thyroid peroxidase, lowering production of T3/T4 in hyperthyroidism. Toxicities include rare agranulocytosis/aplastic anemia.

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21
Q

What are the advantages and disadvantages of propylthiouracil over methimazole?

A

Propylthiouracil does not cross the placenta and methimazole is a teratogen, which makes propylthiouracil ideal in pregnancy. However, propylthiouracil can cause hepatotxicity requiring liver transplant. Propylthiouracil also inhibits peripheral 5’-deiodinases that convert T4 to T3.

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22
Q

What role does demeclocycline have in endocrinology?

A

It is a V2R inhibitor, lowering the effect of ADH on the renal collecting tubules in SIADH. Side effects are Diabetes insipidus (extension effect) and abnormal bone and tooth development (Tetracycline effect).

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23
Q

What is cinacalcet?

A

It binds and sensitizes the Calcium sensors in the parathyroid, causing decreased PTH release. It is used in hypercalcemia due to primary or secondary hyperparathyroidism. Toxicity is from extension: hypocalcemia.

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24
Q

What are H2 Blockers? Names, mechanism, use

A

Cimetidine, Ranitidine, tidines. They are reverible H2R inhibitors, causing reduced parietal cell H+ pumping in the stomach. They are used to treat peptic ulcers, gastritis and GERD. They are best for night-time acidity.

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25
What are the side-effects of H2 Blockers?
They are potent CYP450 inhibitors. They may have antiandrogenic effects by increasing PRL centrally. They compete with Creatinine for renal secretion and cause increase SCr
26
What are Proton ump Inhibitors?
Omeprazole and othe "prazoles". They enter parietal calls and irreversibly inhibit H/K ATPases. They are used in PUD, GERD and Zollinger Ellison Syndrome gastrinoma. By reducing stomach acidity, they increase risk of C. dif infections, pneumonia, and can cause Mg2+ deficiency with chronic use.
27
What is Misoprostol?
It is a PGE analog used to prevent NSAID-induced peptic ulcers. They increase the secretion of gastric mucosa, decrease acid production and counteract the local ischemic effects of NSAIDs on the stomach wall. They may cause diarrhea and uterine contractions (general PGE effects)
28
What is Octreotide?
It is a somatostatin analog that acts centrally to inhibit GH secretion and in the splanchnic vasculature to cause vasoconstriction. It is used for acromegaly before surgery or if not amenable to surgery. It can control variceal bleeds, VIPoma effects, Carcinoid tumor effects.
29
What is Ondansetron?
It is a seratonin 5HT3 antagonist that decreases vagal stimulation causing powerful antiemesis. "an" setronin" It is used to prevent post-surgery vomiting and chemo N/V. As a 5HT antagonist, it can cause Head Ache, constipation, and a prolonged QT interval.
30
What is Metaclopromide?
It is a D2 Receptor antagonist that results in icreased resting tone of the lower esophageal sphicter and increased contractility of the stomach. It is used to treat gastroparesis in DM and post-surgery. Clop inhibits Dop
31
What is Orlistat?
It inhibits pancreatic lipases, to decrease fat absorbtion in the gut. It is used for weight loss. It causes statorrhea and may decrease absorption and deficiency of lipid-soluble vitamins.
32
What are the 1st generation H1 Blockers?
Diphenhydramine, chlorphenirame, dimenhydrinate. They cross the BBB to treat motion sickness, aid sleep. They act peripherally to reduce allergy congestion. They are antimuscarinic, cause sedation and are anti-alphaAR.
33
What are second generation H1 blockers?
Loratidine, ffexofanidine, desloratidine and cetirizine. They do not cross the BBB and only act peripherally to relieve allergy sx. They are less sedating.
34
What is guaifenesin?
It is an expectorant that thins respiratory secretions and has NO effect on the cough reflex.
35
What is N-acetylcystene?
It is a mucolytic that loosens mucous plugs in CF. It is also used as an antidote for acetaminophen OD.
36
What is Dextromethorphan?
It is an codeine analog/NMDA antagonist that suppresses the cough reflex. It can cause 5HT syndrome with MAOIs and other 5HT agonists. OD can be treated with opioid antagonists (naloxone).
37
What are 2 alpha-AR agonists for the tx of nasal congestion?
Pseudoephedrine and phenylephrine. They reduce hyperemia, edema, nasal congestion and can open eustachian tubes. Toxicity includes HTN, CNS stimulation/anxiety and rebound congestion with over-use.
38
What is Bosentan?
It is an endothelin1 antagonist that decreases pulmonary vascular resistance. It is hepatotoxic.
39
What is sildanefil?
It is a PDE5 inhibitor used for ED and pulmonary HTN. It increases cellular cGMP to cause VSMC relaxation.
40
Name 2 Prostacyclin analogs and describe their use.
Iloprost and epoprostanol. They are PGI2 analogs that cause direct vasodilation in pulmonary and systemic arterioles. They also inhibit platelet aggregation. Toxicity includes flushing from vasodilation and possible jaw pain.
41
What is albuterol?
It is a short-acting beta2 agonist used for tx of acute asthma exacerbations.
42
What are salmeterol and formeterol?
They are long acting beta2 agonists used for prophylaxis of asthma exacerbations. Adverse is tremor and arrhythmias.
43
What corticosteroids are used for asthma?
Fluticasone and budesonide. They inhibit NFkB at cytokine production in lungs. They are first line agents for the tx of chronic asthma. They prevent long-term remodeling of the airways.
44
what is ipratropium?
It is a blocker of M receptors ("atropi"), thus preventing bronchoconstriction in asthma and COPD. Tiotropium is the long-acting form.
45
Name 2 LKT receptor blockers.
Monteleukast and zafirleukast. They are particularly useful for aspirin induced asthma.
46
What is zileuton?
It is a 5-lipoxegenase inhibitor to reduce LKT synthesis and minimize resulting bronchoconstriction. It is hepatotoxic.
47
What is Omalizumab?
It is a humanized monoclonal Ab against IgE. It therefore blocks FcRI activation on mast cells. It is used for allergic asthma resistant to steroids and beta agonists.
48
What is Theophylline?
It is a PDE Inhibitor that increases cAMP in bronchiole smooth muscle and causes bronchodilation. It is CYP metabolized and therfor has many DDIs with inducers and inhibitors. It has cardiotoxic and neurotoxic effects.
49
What is methacholine?
It is used in the clinic to induce bronchoconstriction for asthma Dx. It is an M3 R agonist.
50
What is the role of mannitol?
It is an osmotic diuretic. It is filtered by glomeruli but not reabsorbed. It increases tubular osmolarity, thus increasing tubular fluid, flow and GFR. It is used for drug OD to clear renally excreted drugs. It is also used to reduce vascular volume in increased ICP, intraocular pressure.
51
What is acetazolamide?
It is a carbonic anhydrase inhibitor that causes mild sodium bicarb diuresis and lowers total bicarb stores. It is used for glaucoma, urinary alkalinization, metabolic alkalosis, altitude sickness and pseudotumor cerebri. Toxicities are extension effects, including hyperchloremic metabolic acidosis and NH3 toxicity from reduced ability to trap it via proton pumping into the urine. It is a sulfa drug and can cause hypersensitivity or hemolytic anemia in patients with G6PD deficiency.
52
Name 3 Loop Diuretics.
Furosemide, Bumetanide, Torsemide. They are sulfas that inhibit the Na-K-2Cl cotransporter in the LoH. This abolishes much of the hypertonicity of the renal medulla, preventing normal water reabsorption, preventing urine concetration ability. They also cause PGE2 release to vasodilate the afferent arteriole. They are potassium and calcium wasting. They are used for cHF, liver cirrhosis, nephrotic disease and edema. They also are used for hTN and hypercalcemia.
53
What are toxicities of loop diuretics?
OH DANG! Ototox, Hypok, Dehydration, Allergy to sulfas, Nephritis(interstitial), Gout via hyperuricemia.
54
What is ethacrynic acid?
A non-sulfa loop diuretic. It is used in patients with sulfa allergies.
55
What are hydrochlorothiazide and chlorthaladine?
They are thiazide diuretics, acting on NaCl reabsorption in the distal convoluted tubules. They cause decreased Ca excretion. They are used for HTN, hypercalciuria, nephrogenic DI, and osteoporosis. Tox includes hypercalcemia, hypoK metabolic alkalosis, hypoNa, hypergly/lipid/uricemia, sulfa allergies.
56
What are spironolactone and eplerenone?
They are aldosterone reeptor antagonists , acting in the cortical collecting ducts. They prevent aldosterone induced sodium retention and are potasssium sparing. Toxicities include hyperK and spirono has anti-androgen effects.
57
What are Triamterene and amilioride?
They are non-steroid Sodium channel blocckers,a cting int he cortical collecting ducts. They are used to tx hyperaldosteronism, K depletion and cHF.
58
What are ACE inhibitors and their mechanism/use?
Captopril has a short t1/2 for patient tolerance testing. Lisonopril/enalapril and ramipril are used for long-term tx. They inhibit ACE conversion of At1 to At2 in the lungs. Decreased At2 causes decreased vasoconstriction of the efferent arteriole and causes decreased GFR. This ultimately results in natriuresis and decreased blood volume. It also causes systemic vasoldilation, further lowering blood pressure. This decrease the work-load of the heart and the positive feedback cycle of heart failure. Decreased activation of the R-A-S also prevents heart remodeling that further contributes to HF.
59
What are the adverse effects of ACEIs?
Inhibition of bradykinin degradation may cause a dry cough. Angioedema is an autoimmune reaction requiring therapy cessation. Reduced GFR may cause increase Cr. It increases effective lumenal K by slowing tubular flow, causing K retention and hyperK. Over-vsodilation and natriuresis can cause hypotension. They should be avoided in bilateral renal artery stenosis because the reduction in GFR may cause renal failure.
60
What are ARBs?
They are the "sartans". The block At2 at its receptor AtR1 primarily. They do not cause the cough associated with ACEIs. Less frequent angioedema, but still possible.
61
What is Aliskiren?
It is a direct renin inhibitor that prevents the conversion of angiotensinogen to At1. It is used for HTN tx. Toxicities include hyperK, decreased renal function, hypotension. It can not be combined with ACEIs/ARBs.
62
Describe the role of Heparin.
It activates antithrombin, which then degrades activated factors 2 and ten. It is used for immediate anticoagulation in the setting of PE, DVT and MI. LMWH's include parinux, which only act on factor ten. They have better bioavailability, longer half lives and do not require monitoring. However, they are less easily reversed. Protamine sulfate is used to reverse heaparin by binding its negative charge.
63
What is Heparin induced thrombocytopenia?
It is an autoimmune Ab attack on platelets with bound heparin on their surface PF4. It causes platelet activation and areas of thrombosis. The resulting thrombocytopenia then icreases bleeding. increased BT
64
Name 3 anti-2a agents?
Argatroban, Bivalirudin and Dabigatran. They are used for post-HIT anticoagulation.
65
What is the therapeutic role of Warfarin?
It inhibits gamma carboxylation of factors 2,7,9,10, c and S in the liver. VKORC1 alleles affect the rate of warfarin metabolism. It is used for chronic anticoagulation for risk of venous thromboembolism. Vit K is a slow antidote. Fresh frozen plasma is a rapid antidote. It is monitored with PT. Because Protein C and S have the shortest half lives, their is a transient hypercoaguable state that must be bridged with heparin. Warfarin readily crosses the placenta and is a known teratogen.
66
What are the "xabans"?
They are direct Xa inhibitors, used for prophylaxis of DVT, PE and strokes from A. fib. They are an alternative to warfarin except in cases of prosthetic heart valves. They do not require monitoring. There is no antidote.
67
Describe the types and uses of thrombolytics.
Alteplase=tPA, streptokinase from GGS, reteplase(rPA), tenecteplase. They directly activate plasminogen to degrade pre-formed clots and activate factor 2. They cause increased PT and PTT. They are used in early MI, ischemic strokes and severe PEs. They should be avoided with active bleeds. Antidote=fresh frozen plasma and cryoprecipitates.
68
describe the use of Aspirin for its non-anti-inflammatory uses.
It inhibits the formation of TXA2 in platelets via irreversible COX1/2 acetylation. This prevents platelt activation cascades during arterial clot formation. It increase BT. It is used for MI/stroke prophylaxis from atherosclerosis. Tox includes NSAID-induced gastric ulcers, tinnitis and acute renal failure from vasoconstriction. Reye syndrome in kids with viral illnesses. OD causes initial hyperventilation and respiratory alkalosis, followed by metabolic acidosis with respiratory alkalosis.
69
What are ADP-receptor inhibitors?
Ticlopidine, ticagrelor, clopidogrel, prasugrel. They block ADPRs on platelets, preventing Gp2b3a expression necessary for fibrin-linking and aggregation. They are used for tx of acute coronary syndrome, stenting procedures and to reduce the incidence of thrombotic stroke.
70
What are the Gp2b3a inhibitors?
Abciximab, eptifibatide, tirofiban FIBAs. they prevent platelet aggregation. They are used for unstable angina and angioplasty. They cause increased BT and can cause thrombocytopenia.
71
List 2 PDE3 Inhibitors.
Cilostazole, Dipyridamole. They increase cAMP levels in platelets, preventing aggregation and cause vasoldilation. They are used for intermittent claudication, coronary vasodilation, TIA/stroke prevention and angina prophylaxis.

Pharmacology (3 decks)

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