tratamento farmacológico das dislipidemias - uff · tratamento farmacológico das dislipidemias...

Tratamento Farmacológico das

Dislipidemias

Profa. Elisabeth Maróstica

Universidade Federal Fluminense

Dep. Fisiologia e Farmacologia

Disciplina de Farmacologia Básica

Isotretinoína

LIPOPROTEÍNAS

LIPOPROTEÍNAS E TRANSPORTE DE LIPÍDEOS LIPOPROTEÍNAS E TRANSPORTE DE LIPÍDEOS

1

2

3

4

5

5a

5b

5c

6

7

8 9

10

10a

10b

ABC-A1

10c

HMG-CoA

redutase

(LCAT)

CE (ACAT)

(CETP)

LCAT: lecitina coesterol aciltransferase

ACAT: acilCoA coesterol aciltransferase

CETP: Prot. Transferência de Colesteril Ésteres

MVA: Mevalonato

DISLIPIDEMIA E EXAMES LABORATORIAIS

PERFIL LIPÍDICO: (sôro ou plasma c/ heparina)

- Jejum de 12-14hs, evitar exercício intenso(24h) e álcool(72h)

• Colesterol total < 200 mg/dL

• LDL colesterol (LDL-C) < 160 mg/dL (s/ fator de risco)

• HDL colesterol (HDL-C) H: >40 mg/dL; M: >50 mg/dL

• Triglicerídeos <150 mg/dL

Fórmula de Friedewald : LDL-C = CT - HDL-C - TG/5 (* TG/5 = VLDL-C; válida p/ TG <400mg/dL)

Exames específicos (se necessário) :

• LDL-C pequena e densa

• Lipoproteína (a)

• Perfil de Apoproteínas

Treatment Based on LDL-C Levels (NCEP Adult Treatment Panel III Guidelines, 2004)

RISK CATEGORY LDL-C GOAL THERAPEUTIC

LIFESTYLE CHANGE

DRUG THERAPY

Very high risk <70 mg/dl* No threshold No threshold

Atherosclerosis-induced CHD plus one of:

(a) multiple risk factors,

(b) diabetes mellitus,

(c) a poorly controlled single factor,

(d) acute coronary syndrome,

(e) metabolic syndrome

High risk <100 mg/dl* No threshold No threshold

CHD or CHD equivalent

Moderately high risk <130 mg/dl (Optional <100 mg/dl)

≥100 mg/dl ≥130 mg/dl (100-129 mg/dl)a

2+ risk factors

10-year risk: 10%-20%

Moderate risk <130 mg/dl ≥130 mg/dl >160 mg/dl

2+ risk factors

10-year risk <10%

0-1 risk factor <160 mg/dl ≥160 mg/dl ≥190 mg/dl (Optional: 160-189 mg/dl)b

Fármacos para o Tratamento das Dislipidemias

Estatinas

Fibratos

Resinas de troca

Outros: Ezetimiba

Ác. Nicotínico

Óleo de peixe

Rosuvastatina

LDL (SREBPs)

COLESTEROL

Estatinas

monitorar hepatite, miosite e rabdomiólise CK ,ALT

Estatinas

Diminuem risco e taxa de mortalidade p/ cardiopatia isquêmica

* Efeito uricosúrico

Mecanismo de Ação

* Não associar com estatina

Fibratos

*

Outros agentes reguladores de lipídeos

• prurido MEC ação: niacin inhibits the lipolysis of triglycerides by hormone-sensitive lipase, which reduces transport of

free fatty acids to the liver and decreases hepatic triglyceride synthesis. Niacin and related compounds (e.g.,

5-methylpyrazine-2-carboxylic-4-oxide, acipimox) may exert their effects on lipolysis by inhibiting adipocyte

adenylyl cyclase. Niacin stimulates the HM74A (HM74b)-Gi-adenylyl cyclase pathway in adipocytes, inhibiting

cAMP production and decreasing hormone-sensitive lipase activity, triglyceride lipolysis, and release of free

fatty acids. Niacin may also inhibit a rate-limiting enzyme of triglyceride synthesis, diacylglycerol

acetyltransferase 2

(NIACINA)

Outros agentes reguladores de lipídeos

Ezetimiba

Inibe prot. transportadora de colesterol

no intestino (NPC1L1) - absorção

Inibidor de CETP

• Torcetrabipe (em estudo)

HDL-C