B: 21-24 Flashcards

1
Q

Dyslipidemia drugs

A

Atorvastatin
Rosuvastatin
Simvastatin
Ezetimib
Fenofibrate
Colesevelam

Evolocumab, Alirocumab (PCSK9 Inhibitor= inhibits degredation of LDL-R )

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Statins MOA

A

HMG-CoA reductase inhibitors which is the rate limiting step of endogenous cholesterol synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Statins actions

A

Liver cholesterol ↓
LDL-R expression ↑ (liver compensation to clear LDL, vLDL remnants from blood)

HDL ↑ 5-15%
Plasma LDL ↓ (20-50% reduction)

VLDL synthesis by liver ↓
Plasma TG ↓

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Atorvastatin
Rosuvastatin
Simvastatin

Difference

A

Atorvastatin: Active as given
Rosuvastatin: Active as given
Simvastatin: Prodrug

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Atorvastatin
Rosuvastatin
Simvastatin

Metabolism

A

CYP450

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Atorvastatin
Rosuvastatin
Simvastatin

Indications

A

Atherosclerotic vascular disease
Acute coronary syndrome
Reduced risk of cardiovascular disease
Reduced mortality in ischemi heart dieseas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Statins side effects

A

Hepatotoxicity
Myalgia
Rhabdonyolysis

increase creat kinase in 10%

allergy “statin intolerance”

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Statins contraindications

A

Teratogenic
Liver diseas caution

food which inhibit CYP450 eg grapefruit increase hepatotoxicity risk and myopathy.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Colesevelam MOA

A

resin

Bile acid binding resin are

Large non absorbable polymers that bind bile acid and prevent their absorption in intestine –> increase BA in intestiine > GI side effect

this divert hepatic cholesterol to the synthesis of new bile >> decreasing cholesterol in tightly regulated pool

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Bile acid sequestrans drug

A

Colesevelam

colestipol

cholestyramine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Colesevelam how to give and when?

A

Oral
With meals

Dont give togather with other drugs (warfarin, thiazide, digoxin, aspirin, statin) and vitamins (K, folate) (wait btw. 4 h)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Colesevelam indications

A

Primary hypercholesterolemia type IIA (LDL↑)
With Statins

pruritis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Colesevelam side effects

A

VLDL ↑
TG ↑

  • GI: bloat, constipation, diarrhea , Vit. ADEK malabsorption
  • Hyperglycemia
  • Gall stones
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Sterol absorption inhibitors

A

Ezetimibe

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Ezetimibe MOA

A

decrease intestinal absorption by
Block NPC1L1 in intestine
Reduce cholesterol absorption

Liver cholesterol ↓
LDL-R expression ↑
Plams LDL ↓ (20% reduction)

5% increase HDL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

PCSK-9 inhibitors

A

Evolocumab, Alirocumab (PCSK9 Inhibitor= inhibits degredation of LDL-R )

Humanized monoclonal antibody against enzyme PCSK-9, which normally transport LDL-R to lysosomal degradation

  • decreases LDL-R recycling > increase in LDL-R > Decreased LDL
    se: Local rxn at site of injection, URT (flu-like symptoms)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Alirocumab, Evolocumab

indications

A

PCSK-9 inhibitors

  • familial hypercholestermeia
  • resistant hypercholesteremia
  • statin intolerance
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Carbonic Anhydrase inhibitors

A

Acetazolamide

Brinzolamide
Dorzolamid
Methazolamid

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Acetazolamide indicaitons

A
  • Diuretic use if edema+ metabolic alkalosis
  • Glaucoma (topical brinzolamid, dorzolamid)- decreases secretion of H2CO3 by ciliary epi into aquous humor > decreases IOP
  • Mountain sickness: decreases H2CO3 secretion into CSF pro by choroid plexus >> acidosis of CSF> Hyperventilation which protect against high alititude sickness
Innr ear disorder
Urinary alkalosis (alkalinization of urine --\> ppt Ca salt --\> renal stones
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Acetazolamide side effects

A
Metabolic acidosis
Renal stones (due to urine alkalinization)

Rapid tolerance ( 1 week application only)

Renal K+ wasting

paraesthesia

Hyperammonemia in cirhosis ( due to urine alkalinization prevents NH3 > NH4+ > hepatic encephalopathy)

self-limiting diuresis in 2-3 days

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Loop diuretics MOA and names

A

Furosemide

Torsemide
Ethacrynic acid

Inhibition of Na/K/2Cl in the thick ascending limb

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Inhibition of Na/K/2Cl in the thick ascending limb will cause

A

Loss of NaCl
Loss of luminal positive potential (Mg,Ca reab.↓)
K and H wasting
Hypokalemic metabolic alkalosis
XOX-2 ↑ → GFR ↑

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Furosemide drug interactions

A

NSAID’s (Decreases efficacy )

Aminoglycosides (ototoxicity)

Lithium
Digoxin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

How are they different?

furosemide

ethacrynic acid

A

Furosemide is a Sulfa drug
Ethacrynic acid is not a Sulfa drug

BOTH are loop diuretics

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Furosemide indications

A
  • HF
  • pulmonary edema
  • other forms of edema
  • Severe hypercalcemia

HTN
Acute renal failure management

26
Q

Furosemide side effects

A

Sulfa drug
Hypovolemia
Hypokalemic metabolic alkalosis
Ototoxicity
Hypocalcemia
Hypomagnesemia
Hyperuriceria

27
Q

Thiazides diuretics MOA

A

Inhibition of Na/Cl transporter in the distal conv. tubule

28
Q

Hydrochlorothiazide drug properties

A

Sulfa drug
Oral
6-12 h

29
Q

Hydrochlorothiazide drug interactions

A

Digoxin
Avoid in DM

NSAID (efficacy decreased due to inhibition of PG, which are important in maintaining GF)

Gout ( due to hyperuricemia SE)

30
Q

Hydrochlorothiazide indications

A

HTN
mild HF
Hypercalciurea w/stones. (Nephrolithiasis)
Nephrogenic DI

Osteoporosis

31
Q

Hydrochlorothiazide side effects

A

Sulfa

  • Hypokalemic metabolic alkalosis
  • Hyponatremia
  • Hypercalcemia , Hyperuricemia , Hyperglycemia

-hypomagnesmia

Lithium levels ↑

32
Q

Thiazides diuretic drugs

A

Hydrochlorothiazide
Indapamide

chlorothiazide(1957) -parenteral only

chlorthalidone

33
Q

Indapamide indications

A

HTN
Can be combined with ACEi

34
Q

Mannitol
MOA
How to give?
Duration of action

A

Osmotic diuresis
IV
Short

35
Q

Mannitol indications

A
  • solute overload in
    • rhabdomyolysis,
    • hemolysis,
    • tumor lysis syndrome
  • Acute Glaucoma
  • brain edema w/coma
  • Intracranial HTN
36
Q

Mannitol side effects

A
  • hyponatremia followed by Pulmonary edema
  • hypernatremia as H2O excreted
  • headache
  • nausea, vomit

Na imbalance
Acute hypovolemia

37
Q

ENaC inhibitor

A

Amiloride

triamteren

38
Q

Amiloride MOA
How to give?
Duration?

A

ENaC inhibitor
oral !
12-24 h

39
Q

Amiloride indications

A

-Hypokalemia caused by other diuretics

Nephrogenic DM
Liddle’s syndrome

  • usually in combo with thiazide (Na/Cl transporter inhibitor)
  • (book)
40
Q

Amiloride side effects

A

Hyperkalemia

41
Q

ADH antagonist

A

Tolvaptan

Conivaptan

42
Q

Tolvaptan MOA
Receptor preferance
How to give?
Duration?

A

ADH antagonist
V2-R antagonist
parenteral !!
12-24 h

43
Q

Tolvaptan indications

A

SIADH

hyponatremia

44
Q

Tolvaptan side effects

A
  • infusion site rxn
  • demyelination if hyponatremia treated rapidly!!

Polyuria
Thirst
Hypernatremia

45
Q

Antihistamines

H1-r blockers
Types

A

1st gen: Diphenhydramine, Promethazine, Dimetindene
2nd gen: Cetirizine, Fexofenadine, loratidine

3rd gen: desloratidine, levo-citrizine

46
Q

Antihistamines- 1st gen

A

Diphenhydramine
Promethazine
Dimetindene

47
Q

Antihistamines- 2nd gen

A

Cetirizine (zyrtec)
Fexofenadine

loratidine (clarithine)

48
Q

Antihistamines MOA

A

H1-R antagonists

49
Q

Antihistamines- 1st gen
How to give
Duration
Metabolism
Molecule type

A

Oral, parenteral
4-12 h
CYP450
Lipophilic

50
Q

Diphenhydramine indications

A

IgE mediated allergies (hay fever, urticaria, )
Sedative
Antiemetic
Sleep aid
Anti motion sickness
Pregnancy nausea
Acute extrapyramidal symp. (eg. due to antipscychotic)

51
Q

Diphenhydramine side effects

A

Sedation
Antimuscarinic : dry mouth, blurred vision)

a-R inhibatory effect: orthostatic hypotension

Interact with alcohol- Sedation: BZD , Alcohol

52
Q

Promethazine special features

A

Less anti motion sickness effect
More sedative
More autonomic effect

53
Q

Dimetindene special features

A

Treatment of allergic reactions
Minimally cross BBB; milder SE

54
Q

Antihistamines- 2nd gen
What is special about them?

A

H1-R antag. at peripheral
No autonomic or anti motion sickness effect

55
Q

Cetirizine
Fexofenadine

loratidine

How to give
Duration
Metabolism
Molecule type

A

Oral
12-24 h
CYP450
Less lipophilic

56
Q

Cetirizine
Fexofenadine

Indications

A

IgE allergies ( hay fever, angioedema

57
Q

Cetirizine
Fexofenadine

Side effects

A

Sedation
Arrhythmias in overdose
When interact with alcohol- Sedation

58
Q

H2-r blockers

A
  • cimetidine (+weak anti-androgenic effect)
  • ranitidine
  • famotidine
  • nizatidine
59
Q

Histamine analogue name, moa

A
  • beta-histine dihydrochloride:
    • weak H1 agonist
    • H3 antagonist
60
Q

beta-histine indication

A
  • vestibular vertigo
  • menieres syndrome (virtigo+hearing loss)
61
Q

beta-histine MOA

A
  • local vasodialation improves inner ear microcirculation
  • dose-depending inhibiting effect in CNS on spike-generation in vestibular nuclei neurons.
62
Q

beta-histine CI

A
  • peptic ulcer
  • never give histamine + antihistamine