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Pharm - ANTIHYPERTENSIVES

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Pharm - ANTIHYPERTENSIVES Powered By Docstoc
					ANTIHYPERTENSIVES
 See separate notes on Diuretics, Ca++ Channel Blockers!

DRUG               MOA / PHARM                   USES                          SE / Contraind.              NOTES
ACEI’s             Blocks normal actions of      Mildsevere HTN                dry cough (substance P,   Works better in younger
  Captopril        ACE:                          (effective in 40-50% as           PG’s, bradykinin)        Caucasians, less well in
  Benazepril        - AT-I  AT-II              monotherapy)                   angioneurotic edema        elderly blacks
  Enalapril              =>  AT-II                                                (potentially fatal
  Lisinopril             vasoconstriction      Lt heart failure                  swelling of upper resp
  Moexipril              TPR BP                                                  structures)
  Quinapril              =>  Aldosterone       Diabetic nephropathy           neutropenia
  Ramipril               H2O, Na+ retention                                    proteinuria
  Fosinopril
                          vasc                 Advantages:  lyte             glycosuria
                                                 imbalances, increased          hepatotox
                         volumeCO BP
                                                 trigly, insulin resistance,    rash
                    -  inactivation of
                                                 or uric acid accum.
                         bradykinin  blocks                                    CNS problems
                         vasoconstriction                                       GI problems
                    systolic,  diastolic                                     Hypotension

                                                                               CONTRAIND.
                                                                                Pregnancy
                                                                                Renal insuffic.
                                                                                Renal art. stenosis

DRUG               MOA / PHARM                   USES                          SE / Contraind.              NOTES
AT-II Receptor     Binds Type I AT-II receptor   Same as ACEI – appears         Hypotension                Like ACEI, less effective
Antagonist         – blocks only AT-II effects   equally effective              Hyperkalemia (esp. in      in elderly, blacks
   Losartan        (no effect on ACE                                               renal disease)
                   inactivation of bradykinin)   Advantages:                    GI problems
                                                  No cough                     HA, dizziness
                                                  No angio-neurotic
                                                    edema
                                                  Decreased uric acid
                                                    levels
DRUG               MOA / PHARM                           USES                      SE / Contraind.                   NOTES
ADRENERGIC
BLOCKERS

1 Antagonists     Block peripheral post-synaptic 1     Mild severe HTN          - “1st dose” syncope
   Prazosin        receptors vasodilation (arterial +                             - postural
     Doxazosin     venous)                               CHF, but not for LT use     hypotension
     Terazosin                                                                     - palpitations
                   Resistance vessels are affected >>                              - LDL, HDL, trigly
                   capacitance                                                     - CNS effects
                                                                                   - tachyphylaxis in
                                                                                     CHF
2 Agonists        Stimulate postsynaptic inhibitory     - Mild severe              - dry mouth
   Clonidine       neurons in vasomotor ctr  symp        HTN                       - CNS effects
    Guanabenz      outflow from CNS  HR, CO,          - High renin                - Sexual SE’s
    Guanfacine     BP                                     HTN                       - Constipation
    Methyldopa                                           - corrects reflex           - Periph edema
                                                           tachy caused              - Slight/ no effect on lipids
                                                           by vasodilators           - W/ abrupt discontinuation:
                                                         - (Opiate                           Arrythmias
                                                           withdrawal)                       Rebound HTN




1,2 Antagonists   Effects due to 1 block:              - Mild severe            Most due to 2 effects:
   Propanolol       - CO                                  HTN                      - hypoglycemia
     Carteolol      -  renin secretion                  - High renin               - bronchospasm
     Labetalol     Some have Intrinsic                     HTN
     Nadolol       Sympathomimetic Activity (ISA) –      - high CO HTN             Also:
     Pindolol      good for bradycardia                  - HTN w/ angina            - CNS effects
     Timolol                                             - corrects reflex          - Bradycardia
     Penbutolol                                            tachy caused             - CHF
                                                           by vasodilators          - GI SE’s
                                                         - CHF (now standard of     - Raynaud’s Sx
                                                         care!)                    Caution in:
                                                                                    - diabetics
                                                                                    - bronchospasm
                                                                                    - depression
1 Antagonist      See 1,2 - above                      See 1,2 - above           Same as 1,2 – except no 2
   Atenolol                                                                         effects (hypoglycemia,
    Acebutolol                                                                      bronchospasm)
    Betaxolol
    Esmolol
    Metoprolol
Adrenergic Neuron   Reserpine:                            Reserpine:                   Reserpine:
Inhibitors          Inhibits DA, NE uptake @ pre-         Mild mod. HTN                - sedation, depression,
   Reserpine        synaptic neuronDA, NE                                                  nightmares
   Guanethidine     degradation  CO,TPR                Guanethidine:                 - bradycardia
                                                          Severe, refractory HTN        - pseudo-Parkinsonism
                    Guanethidine:                                                       - Crosses BBB and will
                    Mimics Epi, Ne structure  blocks                                       deplete 5HT, DA also!
                    post-ganglionic receptors, causing                                      Don’t use if hx of
                    depletionof stored NE, inhib. of NE                                     depression
                    releaseCO,TPR
                                                                                       Guanethidine:
                                                                                        - postural hypotension
                                                                                        - impotence
                                                                                        - bronchoconstriction
                                                                                        - bradycardia
                                                                                        - fluid retention
                                                                                        (does not cross BBB)
Ganglionic          Competetively inhibits Ach at post-   ?- better agents now exist   Severe!                         IV only; must
Blockers            ganglionic Nicotinic receptor                                      - Hypotension                  monitor
   Trimethaphan     Symp + parasymp block                                              - Parasymp blockade (urine     Closely;
                    CO,TPR                                                                eretntion, constipation,   effects stop as
                                                                                            impotence, dry mouth,      soon as med
                                                                                            visual disturbances)       stopped
DRUG            MOA / PHARM                  USES                       SE / Contraind.              NOTES
VASODILATORS
Hydralazine     ?–                           Hypertensive emergency     Severe!                      Use as triple therapy w/
                increases NO  vasodil?                                   - baroreceptor reflex     diuretic, sympatho-lytic
                Blocks Ca++ influx?                                            tachycardia
                                                                          - palpitations
                - Arterial vasodilation                                   - dizziness, HA
                                                                          - fluid retention
                                                                          - GI SE’s
                                                                          - Precipitates angina
                                                                          - Lupus-like sx: rash,
                                                                               glomerulo-nephritis
Minoxidil       See above                    Severe, refractory HTN     - reflex tachycardia         oral
                                                                        - aggravates angina
                                             (Topical = Rogaine)        - fluid retention
                                                                        - hirsutism
Diazoxide       See above                    Hypertensive emergency     - reflex tachycardia         IV
                                                                        - insulin resistance,
                                                                        hyperglycemia
                                                                        - hyperuricemia
                                                                        - fluid retention

Nitroprusside   Causes NO release from       - Hypertensive emergency    -    severe hypotension     IV
                rbc’s activates guanylate   - post-MI, for LVH          -    myocardial ischemia
                cyclase  cGMP             - severe, refractory CHF    -    thiocyanate toxicity
                arterial and venous          - dissecting AA             -     renin
                vasodilation
                preload, afterload

				
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posted:12/23/2011
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