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systemic pharma- week 2 > Antihyperlipidemics > Flashcards

Antihyperlipidemics Flashcards

1
Q

Main agents used clinicaly to lower lipid levels in the blood?

A

1) statins (1st line)
2) Bile acid resins (3rd line)
3) Niacin, Vitmaine B3 (combo tx w/ statin)
4) Fibrates (2nd line)
5) Other Novel therapies (adjuncts)

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2
Q

Statins exmaples + High intensity statins

A

Simvastatin
Iovastatin
Pravastatin

High intensity:
Atorvastatin
Rosuvastatin

-statin

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3
Q

MoA of Statins

A

HMG-CoA reductase inhibitor–> reduces Heptaic Cholestrol synthesis

-Upregulates LDL receptor synthesis(higher clearnace from plasma into liver cells)

Main biochemical effect:
reduce plasma LDL, SOME reduction in Triglycerides and Increase in HDL

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4
Q

Clinical uses of Statins

A
  • Lower plasma cholesterol
  • Reduce CV events by 25-50%
  • High intensity statins at high doses: might reduce LDL by more than 50%.
  • Secondary prevention of MI and stroke in patients who have atherosclerotic disease.
  • Primary prevention of arterial disease in patients with high cholesterol levels.
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5
Q

Clinical uses of Atrovastatin

*High intensity Statin

A

lowers cholesterol in patients with homozygous
familial hypercholesterolemia

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6
Q

AE of Statins

A

Generally WELL TOLERATED w/ mild AE
1. Rash
2. insomnia
3. Myalgia
4. GI disturbance
5. Hepatoxicity

sever AE:
6. Angioedema
7. Rhabdomyiosits
8. Myopathy

*Rhabdomyiositis: muscle tissue damage

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7
Q

Contraindication of Statins

A
  1. Pregnancy
  2. Gemfibrozil (higher risk of rhabdomyolysis)
  3. CYP450 inhibitors (increase toxicity) like grapefruit
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8
Q

Fibrates Examples

A
  • Bezafibrate
  • Ciprofibrate
  • Gemfibrozil
  • Fenofibrate
  • Clofibrate

-Fibra

* BCCGF (BBC Great Feed)

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9
Q

MoA of Fibrates

A

PPARgamma activation
* ↓ circulating VLDL and Triglycerides
* ↓ Plasma C-reactive protein and fibrinogen
* ↑ LDL hepatic uptake –> by increasing the transcription of lipoprotein lipase, apoA1 and apoA5

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10
Q

Clinical uses of Fibrates

A
  • Mixed dyslipidaemia
  • When hyperuricaemia + mixed dyslipidaemia, use Fenofibrate since it is uricosuric
  • Low HDL and high risk of atheromatous disease
  • combined with other lipid-lowering drugs in patietns w/ sever tx- resistant dyslipidaemia
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11
Q

Clinical uses of Fenofibrate

A

hyperuricaemia + mixed dyslipidaemia

Fenofibrate is Uricosuric

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12
Q

AE of Fibrates

A
  1. Gallstones (especially caused by Clofibrate)
  2. GI symptoms, pruritus and rash are more common
    than statins
  3. Rhabdomyolysis - rarley (occurs to who
    has renal impairments and alcoholics)
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13
Q

Contraindications of Fibrates

A

combination w/ statins (will cause Rhadomyolysis) esp. Gemfibrozil

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14
Q

AE of Clofibrate

A

Gallstones
(use is limited in patients who had a cholecystectomy - removal of gall bladder)

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15
Q

Bile acid-binding resins durg examples

A

Colestyramine
Colestipol
Colesevelam
-Coles (Cholesteol inhibitors)

triple C

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16
Q

MoA of Bile acid-bindings resins drugs

A

Inhibit cholestrol absorption

  • Sequester bile acids in intestine
  • Prevent their reabsorption and enterohepatic recirculation
  • Excretion in faeces
  • Increased metabolism of endogenous cholesterol into bile acids in the liver
  • Increased LDL receptor expression on hepatocytes→less LDL in plasma
17
Q

Clinical uses of Bile acid-binding resins

A
  1. FH patients
  2. Tx bile salt-associated symptoms of Pruritus and diarroea

*FH: familial Hypercholestrolemia

18
Q

AE of Bile acid-binding resins

A

Unacceptable constipation and
bloating

19
Q

Contraindications of Bile acid-binding resins

A
  • With thiazide diuretic, digoxin and warfarin, they interfere with absorption of fat- soluble vitamins.
  • They rise triglyceride levels!!
20
Q

MoA of Ezetimibe

A

Cholesterol absorption inhibitors from
duodenum (blockade of NPC1L1)
°Less LDL stimulates LDL receptor synthesis

21
Q

Clinical uses of Ezetimibe

A

1st choice when combining w/ statins when response has been inadequent

22
Q

Clinical uses of Cloestyramine and Colesevelam

-coles (cholestrol)

A

1) For hypercholestrolemia when a statin is contraindicated
2) Uses unrelated to atherosclerosis including:
- patients with partially biliary obstruction with pruritus and bile acid
- diarrhoea caused by diabetic neuropathy

23
Q

AE of Ezetimibe

A

1) Diarrhoea
2) Abdominal pain
3) rash
4) headache
5) Angio-oedema

24
Q

Clinical uses of Niacin

A

Adjunct to a statin and diet in dyslipidaemia (Especially when ass. w/ low HDL and hight triglycerides)

25
Q

MoA of Niacin, vitamin B3

A

reduces Lp(a) levels
* B3 converted to nicotinamide which inhibits VLDL secretion = reduction in triglyceride and LDL and increase in HDL

26
Q

AE of Niacin, vitamine B3

A

1) Flushing (because of production of PGD2) reduced by aspirin.
2) Palpitations
3) GI disturbance
4) Disturbed liver function

27
Q

Contraindications of Niacins

A

Peptic ulcers, gout
precipitation.

28
Q

MoA of Evolocumab , Alirocumab

*Novel therapies

A

novel therapies
PCSK9 inhibitors (Proprotein Convertase Subtilisin/kexin Type 9)→promotes degradation of LDL receptor in hepatocytes by targeting it for lysosomal degradation

29
Q

Clinical uses of Evolocumab , Alirocumab

A

°Primary hypercholesterolemia, mixed dyslipidaemia;
°In combination with statin when unable to
reach LDL-C goals
°For statin intolerant patients

30
Q

AE of Evolocumab, Alirocumab

A

°Nasopharyngitis
°Upper respiratory tract infections
°Injection-site reactions
°Myalgia
°Cognitive effects

31
Q

MoA of Mipomersen

A

Antisense oligonucleotide for coding region
of apoB-100 mRNA→inhibits synthesis and
apoB-100-containing lipoprotein synthesis

32
Q

Clinical uses of Mipomersen

* novel therapy drug

A

Adjunct treatment for FH

*FH: familial hypercholesterolemia

33
Q

AE of Mipomersen

*Novel therapy drug

A

1) Accumulates in the liver (site of intended action)
2) Hepatotoxic

34
Q

MoA of Lomitapide

*Novel therapy drug

A

Inhibitor of microsomal triglyceride transfer
protein (MTP) which is important in the
assembly and release of apoB-containing
lipoproteins into circulation.–> plasma lipid
levels decrease

35
Q

Clinical uses of Lomitapide

A

Adjunct Tx for FH (oral)

systemic pharma- week 2 (3 decks)

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