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
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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