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PHAR 504 > module 4 drugs > Flashcards

module 4 drugs Flashcards

1
Q

pramlinitide

A
  • amylin analog
  • delays gastric emptying
  • lets T2D reduce their insulin dose
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2
Q

octreotide

A
  • somatostatin analog
  • used to treat hyperglycemia or insulin-secreting tumors
  • will decrease amount of insulin released
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3
Q

glibenclamide, glipizide, glimiperide

A

-secretagogue: sulfonylureas

  • inhibit the K-ATP channels on beta cells in pancreas, depolarizing the cell, Ca2+ comes in, causing release of insulin
  • cause hypoglycemia
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4
Q

Repaglinide, Nateglinide

A

-secretagogue: Meglinitides

  • structurally different than sulfonylureas, but they also bind and inhibit K-ATP channels, causing insulin release
  • rapidly absorbed and cleared, requires multiple daily doses, but also lower risk for hypoglycemia
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5
Q

exenatide, liraglutide

A

-secretagogue: GLP-1 receptor agonists (incretin mimetic)

  • they act like the gut hormones and potentiate glucose-dependent secretion of insulin
  • side effect: acute pancreatitis
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6
Q

Gliptins

A

-secretagogue: DPP-4 inhibitors (incretin mimetics)

  • inhibit DPP4 which breaks down the incretins
  • potentiate glucose-dependent secretion of insulin by potentiating endogenous incretins
  • possible pre-cancerous changes in the pancreas?
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7
Q

Metformin

A

Sensitizer: Biguanide

  • lowers blood glucose by decreasing hepatic glucose output and sensitizing peripheral tissues to insulin.
  • increases glucose uptake and utilization in skeletal muscle
  • does not cause hypoglycemia because insulin secretion is not altered
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8
Q

Pioglitazone, Rosiglitazone

A

-Sensitizers: the glitazones (aka TZDs)

  • bind to nuclear receptors and alter transcription of genes that enhance function of insulin receptors and signaling (like Glut-4)
  • slow onset (1-2 months)
  • used in combination w sulfonylureas, metformin, or insulin
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9
Q

Acarbose, Miglitol

A
  • alpha glucosidase inhibitors
  • MOA: inhibit the alpha-glucosidase enzymes that line the brush border of the s.i., interfering with the hydrolysis of carbohydrates and delaying absorption of glucose
  • only lower AIC by 0.5%-1.0%
  • drug taken w each meal to lower post-prandial glucose concentrations
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10
Q

Canagliflozin, Dapagliflozin

A

-Sodium glucose co-transporter 2 (SGLT-2) inhibitors

  • SGLT2 is a membrane protein in kidney that transports glucose from proximal tubule into tubular epithelial cells
  • SGLT2 inhibitors decrease renal glucose reabsorption and increase urinary glucose excretion
  • weight loss drug
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11
Q

pramlinitide

A
  • amylin analog
  • delays gastric emptying
  • lets T2D reduce their insulin dose
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12
Q

colesevelam

A

a bile-acid sequestrant used to lower LDL cholesterol

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13
Q

Bromocriptine

A

DA agonist

  • modestly effective at decreasing blood glucose levels in T2DM
  • safer cardiovasvular profile
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14
Q

Orlistat

A
  • pancreatic and gastric lipase inhibitor that decreases fat absorption
  • SI: flatulance with discharge, oily spotting, fecal urgency
  • ~ 3 kg loss
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15
Q

Lorcaserin

A
  • 5-HT- 2C agonist
  • works on the POMC neurons –> they release alpha MSH, signals to satiety center = more full
  • SI: cardiac valvulopathy, serotonin syndrome
  • ~ 3 kg loss
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16
Q

Liraglutide

A

insulin secretagogue… GLP1 agonist

  • decreases gastric emptying
    loss: 5.8 kg
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17
Q

Benzphetamine, Diethylpropion, Phentermine, Phendimetrazine, QYSMIA

A

sympathomimetic amines

  • reduce appetite by eliciting norepinephrine release, and by modulating other catecholamine systems
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18
Q

off label treatments

A

antidepressants, antiepileptics, antihyperglycemics

19
Q

Zonisamide

A

antiepileptic drug
3.3 kg loss
zonisamide + olanzapine prevented weight gain normally seen with olanzapine

20
Q

anti-hyperglycemics

A

exenatide- GLP1 agonist. stimulates glucose dependent insulin secretion. ~ 4 kg weight loss seen.

metformin- biguanide. modest but sustained weight loss

pramlinitide- weight loss bc delays gastric emptying

SGLT2 inhibitors- pee out the glucose

21
Q

Statins

A
  • specific, reversible, Hmg-CoA reductase inhibitors
  • prevent synthesis of cholesterol
  • increase expression of LDL receptors, increasing uptake of LDL
  • longer acting : Atoravastatin, Rosuvastatin
22
Q

ciprofibrate, gemfibrozil, etc

A

Fibrates (fibric acid derivatives)

  • influence transcription of genes beneficial to prevent atherosclerosis
  • fibrates bind PPAR alpha –> activated PPAR/RXR complex –> PPAR response elements =
  • decrease VLDL, decrease TG, decrease inflammation
  • increase LDL size, increase HDL synthesis, increase reverse cholesterol transport
23
Q

Colestyramine, colestipol, colesevelam

A

bile acid sequestrants (resins)

  • bind to bile acids with cholesterol and cholesterol gets excreted
  • decreased LDL levels
24
Q

Ezetimibe

A

(fancier version of a resin)

  • impairs dietary and biliary cholesterol absorption at brush border without affecting fat-soluble vitamins)
  • reducing the pool of cholesterol absorbed from diet –> less cholesterol available to the liver
  • upregulate LDL receptor, so LDL levels in the blood decrease
25
Q

Vytorin

A

ezetimibe/ simvastatin

dual inhibitory effect

26
Q

nicotinic acid

A

Niacin (vitamin)

  • used in gram quantities
  • converts itself to nicotinamide, which inhibits hepatic VLDL secretion = reducing LDLs and TGs
27
Q

Fish oil derivatives

A

long chain omega 3 fatty acids (PUFA) (second line therapy)

  • inhibition of HSL and VLDL secretion
  • increase LPL activity, decrease TGs
28
Q

Alirocumab, Evolocumab

A
  • PCSK9 inhibitors

prevent degradation of LDL receptors

29
Q

anti-platelets

A
  • COX inhibitors
  • PDE inhibitors
  • ADP inhibitors
  • GpIIa-IIIb antagonists
  • thrombin receptor antagonists
30
Q

aspirin

A
  • COX inhibitor
  • aspirin inhibits the synthesis of prostaglandins, inhibiting the platelet granule release reaction- interfering with normal platelet aggregation
  • used to prevent thrombosis
  • used in low/ intermittent doses
  • NSAIDs covalently acetylate a serine residue on COX enzyme near the active site –> blocking effects of TxA2
31
Q

Dipydramole

A
  • PDE inhibitor

- blocks the reuptake of adenosine… increases cAMP… decreasing platelet aggregability

32
Q

“The Grels” … Clopidogrel, prasugrel, ticagrelor, annnnd (Ticlopidine)

A

P2Y-12 ADP receptor inhibitors

  • P2Y receptors are Gi coupled –> decrease cAMP
  • we want to antagonize them bc we want to increase cAMP to decrease platelet aggregability
  • another why: ADP receptors mediate platelet shape change and expression of functional GpIIb-IIIa… we dont want that
33
Q

Abciximab, eptifibatide, tirofiban

A

GpIIb-IIIa antagonists

- stops the crosslinking of platelets… they prevent fibrinogen binding to the GpIIb-III1 receptor

34
Q

Voraxapar

A

thrombin receptor antagonist (PAR1 selective)

- inhibits thrombin’s ability to excise the N-terminus thats silencing platelet aggregation

35
Q

Warfarin

A
  • warfarin inhibits epoxide reductase, preventing vitamin K from being in its reduced, active form.
  • vitamin K is required for 4 coagulation factors: II, VIII, IX, and X, as well as proteins C and protein S
  • oral drug, 100% bioavailable, 36 hr half life
36
Q

drugs that diminish warfarin’s anticoagulant effect

A
  • colestyramine
  • vitamin K (reduced, active form)
  • barbiturates, carbamazapine, phenytoin, rifampin
  • these drugs would decrease the INR
37
Q

drugs that enhance warfarin’s anticoagulant effect

A
  • antifungals
  • antibiotics
  • ethanol
  • steroids, testosterone
  • chloral hydrate
  • amiadarone
  • clopidogrel
  • these drugs would increase the INR
38
Q

Heparins

A
  • lets the anti-thrombin III reaction happen (speeds it up by 1000x)
  • highly negative charge- making it a sticky molecule
39
Q

unfractionated heparins

A
  • can bind simultaneously to thrombin and anti-thrombin III, inactivating both thrombin and Factor Xa by anti-thrombin III
  • monitoring with aPTT: activated partial thromboplastin time (tests the intrinsic & common pathways)
40
Q

low molecular weight heparins

A

can inactivate Factor Xa
is ehhhh at inactivating thrombin
- the parns/ parins

41
Q

rivaroxaban, apixaban, edoxaban

A
  • direct factor 10 inhibitors
42
Q

direct thrombin inhibitors

A
  • derived from medicinal leech protein hirudin
43
Q

tissue plasminogen activator

A
  • t-PA is a serine protease produced by intact endothelial cells, therefore not antigenic
  • t-PA binds to thrombus/ clot with high affinity, undergoes conformational change making it a plasminogen activator, causing fibrinolysis

PHAR 504 (3 decks)

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