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A233 L10-11, Lipoprotein Transport, Intestinal cells, Chylomicron remnants…

- - - - For patients with
        
        Hypercholesterolemia
        
        Mixed dyslipidemia
      - prefix: Statin
        
        Simvastatin
        
        metabolized by CYP3A4
        
        Atorvastatin
        
        Lovastatin
        
        Rosuvastatin
      - Adverse effects
        
        Rhabdomyolysis
        
        Raised liver enzymes
        
        Myopathy
        
        Juandice
    - - For patients with
        
        hypercholesterolemia
        
        Mixed dyslipidemia
      - Example
        
        Ezetimibe
        
        azetidinone cholesterol absorption inhibitors
        
        Blocks transport protein NPC1L1 in the jejunum
        
        substitute for resins and a supplementary treatment for statins
        
        Adverse effects
        
        abdominal pain
        
        headache
        
        Diarrhoea
        
        myalgia
    - - Treatment for
        
        hypercholesterolaemia
        
        mixed dyslipidemia
      - Example
        
        Cholestyramine
      - Sequester bile acids, prevents their reabsorption
      - Adverse effects
        
        Diarrhea
        
        Hypertriglyceridemia
        
        Constipation
    - - Example
        
        Fenofibrate
        
        Gemfibrozil
      - Pharmacokinetics
        
        Decrease circulating VLDL
        
        by increasing gene transcription of
        
        Lipoprotein lipase
        
        apoA1 and apoA2
        
        Increase HDL
        
        Decrease VLDL
        
        By decreasing gene transcription of
        
        apoC2 and apoC3
        
        increased hepatic LDL uptake
      - Treatment for
        
        hypertriglyceridemia
        
        severe hypertriglyceridemia
        
        mixed dyslipidaemia
      - Adverse effects
        
        Myopathy
        
        Lithiasis
        
        Raised liver enzymes
    - - rich in
        
        eicosapentaenoic acid
        
        docosahexaenoic acid
      - treatment for
        
        hypertriglyceridemia
        
        severe hypertriglyceridemia
      - pharmacokinetics
        
        reduce plasma triglycerides
        
        in some
        
        increases LDL by converting VLDL to IDL then LDL
        
        reduce hepatic VLDL production and increases its clearance
      - When taken with PUFA
        
        improves survival of myocardial infarction patients
      - omega 3 fatty acid ethyl esters
        
        treatment for MI and hypertriglyceridaemia
- - - - 2) Lipid accumulation
        
        3) Inflammation
        
        4) Fibrous cap formation
        
        5) Plaque rupture
        
        6) Blood clot formation
    - - peripheral artery disease
        
        coronary artery disease
        
        carotid artery disease
        
        aneurysms
        
        chronic kidney disease
- - - - Competitively inhbits ACE enyme to stop angiotenin I to angiotensin II conversion
      - Examples
        
        Enalapril
        
        Lisinopril
      - Adverse Effects
        
        Angioedema
        
        Persistent dry cough
        
        Hyperkalaemia
    - - Antagonizes AT1 receptors in ateriolar smooth muscle and adrenal gland
        
        Causes arteriolar dilation and increase Na excretion. Decrease blood pressure
      - Examples
        
        Valsartan
        
        Losartan
      - Adverse Effects
        
        Angioedema
        
        Hyperkalaemia
        
        Low incidence of dry cough
    - - Bind to either beta 1 or beta 2 receptors to exert no intrinsic activity
        
        Beta 1 receptors primarily on heart.
        
        Beta 1 blockade reduces heart rate, renin secretion, vasuclar smooth muscle contraction
        
        Beta 2 receptors primarly on airway smooth muscles.
        
        Beta 2 blockade leads to bronchocontriction and vasoconstriction
      - Examples
        
        Beta 1 selective
        
        Atenolol
        
        Biosoprolol
        
        Metoprolol
        
        Non selective (avoided for asthma patients)
        
        Carvedilol
      - Adverse Effects
        
        Bradycardia
        
        Reduced cardiac output
        
        Hypoglycaemia
        
        Bronchoconstriction
    - - Block Ca2+ entry by preventing opening of voltage gated calcium channels
        
        Lowered Ca2+ levels decreases contractility of cardiac and smooth muscle and reduces oxgen demand. Decrease blood pressure
      - Examples
        
        Dihydropyridines - primarily affects peripheral circulation
        
        Amlodipine
        
        Nifedipine
        
        Adverse Effects
        
        Peripheral edema
        
        Non-dihydropyridines - affects heart and blood vessels
        
        Verapamil (cardio selective)
        
        Diltiazem
        
        Adverse Effects
        
        Antidysrhythmia
        
        Angina
        
        Bradycardia
        
        Constipation
    - - Increases the amount of urine produced in the kidney
      - Most diuretics with a direct action on the nephron act from within the tubular lumen and reach their sites of action by being secreted into the proximal tubule
      - Diuretics increase the excretion of Na+ and water which reduces blood volume, by decreasing the reabsorption of Na+ and usually Cl− from the filtrate
      - Loop diuretics – act on thick ascending loop of Henle
        
        Thiazide diuretics – act on early distal tubule
        
        Potassium-sparing diuretics/ aldosterone antagonists – act on collecting tubules and ducts
      - Dizziness, Headaches, Dehydration, Muscle cramps, Joint disorders (gout), Impotence,Hypokalaemia
    - - α1 selective antagonist cause vasodilatation through blocking alpha1 receptors on arterioles and veins which causes a fall in arterial pressure by dilating both resistance and capacitance vessels
      - Side effects:Postural hypotension,Reflex tachycardia,Nasal congestion
    - - It is taken up by noradrenergic neurons. Which converts the drug into a-MeNA, displacing NA+. a-MeNA Is less active compared to NA+ reducing vasoconstriction. Bring the NT release to below normal levels which reduces sympathetic outflow to blood vessels and to the heart.
      - Side effects:
        Drowsiness
        Rebound hypertension
    - - Reduce pressure by relaxing arteriole smooth muscles thus reducing peripheral vascular resistance
    - - Renin inhibitors bind to the active site of renin and inhibit the binding of renin to angiotensinogen, which is the rate-determining step of the RAAS cascade. Consequently, renin inhibitors prevent the formation of Ang I and Ang II.
      - Side effects: Diarrhea, hyperkalemia, dizziness, arthralgia
- - - - Renin converts angiotensinogen to angiotensin I
        
        ACE found in pumonary capillaries converts angiotensin I to angiotensin II (active)
        
        Arteriole vasoconstriction
        
        Stimulate SNS to increase heart rate and stoke volume
        
        Increased aldosterone secretion by adrenal cortex
        
        Reabsorption of Na+, Cl-, water. Excretion of K+
        
        Release of vasopression/ADH by posterior pituitary gland to reabsorb water at collecting ducts
  - - - If blood pressure decreases, baroreceptors decrease PNS and increase SNS activity
        
        Increase cardiac output, vasoconstriction
      - If blood pressure increases, baroreceptors increase PNS and decrease SNS activity
        
        Decrease cardiac output, vasodilation
- - - - 6) HDL absorbs excess cholesterol and transports to the liver for use or disposal
        
        HDL