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Hypertension - Coggle Diagram

- - - - Prodrugs eleminated by th kidneys
        
        50% with mild-moderate HTN hotrolled with ACE alone
        
        Young patients with high renin
        
        Move towards earlier dual therapy
        
        90% with mild-moderate HTN controlled with ACEi + Ca2+ channel blocker / β Blocker / diuretic
        
        Diuretics augment the antihypertensive effect of ACE inhibitors
      - Dosing
        
        Enalapril
        
        Initiating : 5-10mg
        Maintenance : 20mg
        
        Lisinopril
        
        Initiating: 10mg
        Maintenance : 10-20mg
        
        Ramipril
        
        Initiating: 2.5-5mg
        Maintenance: 5-10mg
        
        Perindopril
        
        Initiating: 5mg
        Maintenance: 5-10mg
      - Adverse Effects
        
        Hypotension :tent::arrow_down:
        
        First dose effect
        Particularly increased plasma renin activity
        
        Hyperkalaemia :banana:
        
        Associated with renal insufficiency, K supplements, K sparing diuretics, NSAIDs
        
        Acute Renal Failure
        
        In presence of bilateral reanl artery stenosis, volume depletion due to diuretics, older patients with CCF
        
        Fetopathic potential :spider:
        
        Once pregnancy is confirmed, discontinue
        
        Cough
        
        5-10%
        
        Bradykinin
        
        Skin rash
        
        Maculopapular skin rash
        
        Angioedoma
        
        Neutropenia
        
        Dysgeusia
        
        Alteration or loss of taste (catopril)
      - Interactions
        
        NSAIDs
        
        Asipirin may reduce antihypertensive effect
        
        Digoxin / litihum
        
        Increases plasma levels of digoxin / lithium
    - - MOA
        
        Biological effect of angiotensin II via AT1 receptor
        
        ARBs bind to AT1 in blood vessels + adrenal gland with >10,000x selectivity vs AT2
        
        Effects:
        
        Contraction of vascular smooth muscle
        
        Aldosterone secretion
        
        Catecholamine release
        
        Enhances noradrenergic neurotransmission
        
        Increased sympathetic tone
      - Dosing
        
        Losartan
        
        I: 50mg
        M: 50-100mg
        
        Valsartan :mountain:
        
        I: 80mg
        M: 80-320mg
        
        Olmesartan
        
        I: 10mg
        M: 20-40mg
        
        Candesartan :candy:
        
        I: 8mg
        M: 8-16mg
        
        Telmisartan
        
        I:40
        M: 40-80mg
      - Adverse effects
        
        Hypotension
        
        Hyperkalaemia :banana:
        
        Acute renal failure
        
        Fetopathic potential :spider:
        
        Angioedeoma :balloon:
  - - - MOA
        
        Inhibits influx of Ca2+ L-type channels
        
        Inhibits smooth muscle contraction
      - Effects
        
        Antihypertensive
        
        Anti-anginal
        
        Anti-arrhythmic
        
        Cardiac
        
        Decreased contractibility
        
        Decreased HR
        
        Decreased conduction velocity
        
        Valvular
        
        Smooth muscle relaxation
      - Effective monotherapy
        
        Mild-moderate hypertension
        
        Useful in elderly / black population with low renin status
        
        Dihydropyradines with long half life (Amlodipine)_more prolonged antihypertensive effect + less reflex tachycardia than nifedipine
      - Adverse Effects
        
        Amlodipine
        
        Hypotension
        Headache
        Peripheral oedema
        Constipation
        
        Verapamil
        
        Cardiodepression
        Hypotension
        AV block
        Peripheral oedema
        Headache
        Constipation
        
        Diltiazem
        
        Hypotension
        Peripheral oedema
        AV node block
        Cardiodepression
      - Interactions
        
        CYP 34A inhibitors
        
        Increase CCB con.
        
        Ketoconazole
        Ritonavir
        Clarithromycin
        Erythromycin
        
        CYP 3A4 inducers
        
        Reduce CCB conc
        
        Phenytoin
        Carbamazepine
        Rifampicin
        
        β Blockers
        
        With non-dihydropyridines may result in bradycardia or heart block
        
        Digoxin - Verapamil
        
        Verapamil inhibits PgP transporter - inhibits elimination of digoxin
        
        DOACs - Verapamil
        
        PgP inhibition increases plasma conc.
      - Verapamil
    - - Sodium Nitroprusside
        
        Use
        
        Hypertensive emergencies in ICU setting
        
        RoA
        
        IV
        Onset of 30s
        Peak effect 2min
        Effect disappears 3 min after discontinuation
        
        Decomposes under alkaline conditions or when exposed to light
        
        Adverse Effects
        
        Hypotension
        
        Lactic acidosis from accumulation of cyanide and thiocyanacte
      - Hydralazine
        
        MOA
        
        Direct acting relaxation of arteriolar smooth muscle via Nitric Oxide release
        
        Pharmacokinetics
        
        Acetylation in liver
        
        Adverse effect
        
        Hypotension
        
        Palpatations
        
        Flushing
        
        Hyperdynamic circulation - Start a β Blocker first!!
        
        Immunological reactions eg drug induced lupus syndrome
        Fever
        Arthralgia
        
        Use
        
        Resistant Hypertension when other options exhausted - hypertensive emergencies
        
        RoA
        
        IV infusion 50-150μgm/min
      - MOA
        
        Activates Guanylyl cyclase
        
        GC convrts GTP tocCMP
        
        cGMP activates Protein kinases that activates MLC phosphatase
        
        MLC phosphatase dephosphorylates Myosin LC, reducting crossbridge formation and contraction
        
        Causes smooth muscle contraction by inhibing crossbridge formation
      - Glyceryl Trinitrate
        
        Use
        
        Hypertensive emergencies :arrow_up: :tent:
        
        Acute stroke
        
        RoA
        
        IV
        
        Patch
        
        Sublingual
        
        Adverse effects
        
        Hypotension
        
        Headache
    - - Potassium channel openers
        
        Examples
        
        Minoxidil
        
        Prodrug causes arterial vasodilation by opening K+ channels
        
        Adverse Effects
        
        Fluid and salt retention
        
        Reflex tachycardia
        
        Hypertrichosis (abnorma hair growth)
  - - - Examples
        
        Frusemide
        
        Bumetanide
      - MOA
        
        Block Na/K/Cl transporter in thick ascending Loop of Henle
      - Effects
        
        Diuresis and Naturesis
      - Route
        
        Oral
        
        IV for furosemide
      - Adverse effects
        
        Hyponatramia met alkalosis :peanuts:
        
        Hypokalaemia :banana:
        
        Hypocalcaemia :skull_and_crossbones:
        
        Renal Failure
    - - Thiazide Diuretics
        
        Bendroflumethiazide
        
        Hydrochlorothiazide
      - Thiazide-like Diuretics
        
        Chlorthalidone
        
        Indapamide
        
        Metolazone
      - MOA
        
        Blocks Na/Cl transporter in distal convoluted tubule
      - Effects
        
        Diuresis and Naturesis
      - Adverse Effects
        
        Hyponatraemia :peanuts:
        
        Hypokalamic met alkalosis :banana:
        
        Hyperglycaemia in diabetics :candy:
        
        Hyperlipidaemia
        
        Increase in uric acid
        
        Hypercalaemia :skull_and_crossbones:
    - - Examples
        
        Spironolactone
        
        Eplerenone
      - MOA
        
        Blocks aldosterone sensitive Na reabsorption in distal segment of distal tubule
      - Effects
        
        Mild diuresis and Naturesis
      - Route
        
        Oral
      - Adverse effects
        
        Hyperkalaemia :banana:
        
        Metabolic acidosis :lemon:
        
        GIT upset
        
        Gynaecomastia
        
        Sexual dysfunction
    - - Carefully Losing The Plentiful Urine
        
        Carefully
        
        Carbonic Anhydrase Inhibitors
        
        Inhibit Carbonic Anhydrase
        
        Losing
        
        Loop Diuretics
        
        L Loaded NA-K-2Cl symporter
        
        The
        
        Thiazide Diuretics
        
        Thin symporter - only transports Na-Cl
        
        Plentiful urine
        
        Potassium-Sparing Diuretics
        
        Prinicple cells Na+ channel (EnaC) and Aldosterone receptors
  - - - Methyldopa
        
        MOA
        
        Prodrug Metabolised to α-methylnoradrenaline
        
        Substitutes NA
        
        Acts in CNS to inhibit adrenergic outflow from barinstem
        
        Adverse Effects
        
        Sedation
        
        Dry mouth
        
        Reduced renin
        
        Parkinsonism
        
        Hyperprolactinaemia
        
        Gynaecomastia
        
        Galactorrhoea
        
        Hepatotoxicity
        
        Haemolytic anaemia
        
        Use
        
        Hypertension in pregnancy
        
        In guidelines labetalol or nifedipine more often used in practice
      - Clonidine
        
        MOA
        
        Centrally acting α2 agonist
    - - Doxazosin
        
        MOA
        
        Selective α1 blocker
        
        Pharmacokinetics
        
        20hr half life
        
        Dose 1mg - 16mg OD
        
        Adverse Effects
        
        Hypertension - 1st dose in 50% pts
        
        Dizziness
        
        Headache
        
        Oedema
        
        Fatigue
        
        May reduce LDL cholesterol and TG, increase HDL
        
        Consider carefully in elderly
        
        Not first line theapy but ,ay be in combination with other antithypertensives
      - β Blockers
        
        Examples
        
        Bisoprolol
        
        Non-selective
        
        Nebivolol
        
        Atenolol reducing
        
        Labetalol
        
        Carvedilol
        
        Propranolol
        
        Timolol
        
        MOA
        
        Relative affinity for β1 and β2 receptors
        Blockade of α receptors
        
        Intrinsice sympathomimetic activity (ISA)
        
        Inhibit renin release from JGA
        
        Inhibit β1 receptors, reducing HR, contractiliy and CO
        
        β1 selectivity results in less effect of smooth muscle (asthma, COPD)
        
        Adverse Effects
        
        Bronchocontriction
        
        Interactions with drugs that impair sinus node/ AV function (verapamil)
        
        Blunt recognition of hypoglycaemia
        
        CNS
        Fatigue
        Sleep disturbance
        
        Rebound hypertension in discontinuation
        
        Contraindications
        
        Asthma / COPD
        
        Peripheral vascular disease
        Raynaud's syndrome