Pharmacology

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Author:
jknell
ID:
113218
Filename:
Pharmacology
Updated:
2011-10-30 19:09:06
Tags:
Adrenergic
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Description:
Adrenergic drugs
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  1. Drugs that affect NE synthesis and storage
    • 1. alpha-Methyltyrosine
    • 2. alpha-Methyldopa
    • 3. Reserpine
  2. alpha-Methytyrosine
    Mechanism: Inhibits tyrosine hydroxylase

    Major Indications: Pheochromocytoma

    Adverse Effects: Drowsiness, Depression
  3. alpha-Methyldopa
    Mechanism: Prodrug, Converted to alpha-MethylNE (replaces NE)

    Major Indications: HTN

    Adverse Effects: Sedation, xerostomia

    Other: alpha-MeNE is an a2 agonist (HTN effects)
  4. Reserpine
    Mechanism: blocks VMAT-2 (depletion of NE in synaptic vesicles)

    Major Indications: HTN

    Adverse Effects: extreme sedation, severe depression, diarrhea, nasal congestion

    Other: seldom used
  5. Drugs that affect NE release
    • Indirect Sympathomimetics
    • 1. Amphetamine
    • 2. Ephedrine (Sudafed)
  6. Amphetamine
    Mechanism: uptake by NET and then by VMAT, displacing NE into the junctional space

    Major Indications: ADHD, narcolepsy

    Adverse Effects: drug abuse, increase BP HR and cardiac arrythmias, insomnia, headaches, nervousness
  7. Ephedrine
    Mechanism: uptake by NET and then by VMAT, displacing NE into the junctional space

    Major Indications: Hypotension, nasal congestion (pseudoephedrine)

    Adverse Effects: increase BP and HR, insomnia, nervousness

    Other: weak agonist effects an Beta receptors
  8. Drugs affecting NE reuptake
    • 1. Tricyclic anti-depressants (Amitriptyline)
    • 2. Cocaine
  9. Amitriptyline
    Mechanism: inhibit NET (NE stays in NEJ)

    Major Indications: depression, neuropathic pain, migraine prophylaxis

    • Adverse Effects:
    • -mAChR antagonistic side effects (dry mouth, urinary retention, confusion)
    • -alpha1 antagonist effects (postural hypotension)
    • -H1 antagonist effects: sedation, increase weight gain
    • -Cardiac arrythmias

    Other: low therapeutic index (overdose)
  10. Cocaine
    Mechanism: Inhibit NET (NE in NEJ)

    Indications: drug of abuse

    Adverse effects: increase BP, HR and cardiac arrhythmias
  11. Drugs inhibiting NE metabolism
    1. MAO inhibitors

    2. COMT inhibitors
  12. MAO Inhibitors
    Mechanism: inhibit MAO (NE metabolism)

    Indications: depression, Parkinson's

    Adverse Effects: HTN crisis when ingest tyramine-containing foods
  13. COMT Inhibitors
    Mechanism: inhibit COMT (NE metabolism)

    Indications: Parkinson's
  14. Endogenous catecholamines as drugs
    • 1. NE
    • 2. Epi
  15. NE as a drug
    Mechanism: stimulates a1, a2 and b1 receptors

    Indications: Severe hypotension, shock (to increase BP)
  16. EPI as a drug
    Mechanism: stimulates a1, a2, b1 and b2 receptors

    Indications: acute anaphylactic reactions, cardiac arrest (maintain BP), severe hypotension, shock, local anesthesia (increased duration of action by decreasing blood flow to area)

    Other: given at relatively high dose so a receptor vasoconstriction predominates of b2 receptor vasodilation
  17. a1-selective agonists
    Phenylephrine
  18. Phenylephrine
    Mechanism: stimulate a1 receptors

    Indications: Nasal congestion, opthamalogical exam (mydriasis)

    Adverse Effects: increase BP

    Other: use with caution in Pt with HTN and BPH
  19. a2-selective agonists
    Clonidine
  20. Clonidine
    Mechanism: stimulates a2 receptors

    Indications: HTN

    Adverse Effects: sedation, xerostomia

    Other: anti-HTN effects primarily due to stimulation of a2 receptors on medulla oblongota (decreases sympathetic tone)
  21. Non-selective a receptor antagonists
    Phentolamine
  22. Phentolamine
    Mechansim: blocks a receptors

    Indications: pheochromocytoma

    Adverse Effects: postural hypotension with reflex tachycardia
  23. a1-selective antagonists
    • 1. Prazosin
    • 2. Tamsulosin

    '-osins'
  24. Prazosin
    Mechanism: blocks a1 receptors

    Indications: HTN, BPH

    Adverse Effects: Postural hypotension, with reflex tachycardia
  25. Tamsulosin
    Mechanism: blocks a1 receptors

    Indications: BPH

    Adverse Effects: postural hypotension with reflex tachycardia

    Other: causes less hypotension
  26. Non-selective b agonist
    Isoproterenol
  27. Isoproterenol
    Mechanism: stimulates b receptors

    Indications: extreme bradycardia and AV block

    Side Effects: tachycardia, cardiac arrhythmias, angina pectoris

    Other: used in emergency situations
  28. b1-selective agonists
    Dobutamine
  29. Dobutamine
    Mechanism: stimulates b1 receptors

    Indications: Cardiogenic shock

    Other: increases ionotropic state more than HR
  30. b2-selective agonists
    Albuterol
  31. Albuterol
    Mechanism: Stimulates b2 receptors

    Indications: Asthma, COPD

    Adverse Effects: tremor, anxiety, apprehension, cardiac stimulation (not 100% selective)

    Other: administer by inhalation to reduce side effects
  32. Non-selective b antagonists
    Propranolol
  33. Propanlol
    Mechanism: block b receptors

    Indications: HTN, angina pectoris, MI, CHF, cardiac arrhythmias, glaucoma, essential tremor, performance anxiety, migraine prophylaxis

    Side Effects: CH, bradycardia, AV block, bronchoconstriction, fatigue, sleep disturbance, depression, impair peripheral circulation (b2 receptors), sexual dysfunction in males, increased risk of hypoglycemic episodes in diabetes, increase risk of sudden death and exacerbation of angina pectoris with discontinued use
  34. b1- selective antagonists
    • 1. Metoprolol
    • 2. Atenolol

    (A-N -olols)
  35. Metoprolol
    Atenolol
    Mechansim: blocks b1 receptors

    Indications: HTN, angina pectoris, MI, CHF, cardiac arrhythmias, glaucoma, essential tremor, performance anxiety, migraine prophylaxis

    Side Effects: CH, bradycardia, AV block, bronchoconstriction, fatigue, sleep disturbance, depression, impair peripheral circulation (b2 receptors), sexual dysfunction in males, increased risk of hypoglycemic episodes in diabetes, increase risk of sudden death and exacerbation of angina pectoris with discontinued use
  36. Carvediolol
    Mechanism: block b receptors with additional CV actions (vasodilation)

    Indications: HTN, angina pectoris, MI, CHF, cardiac arrhythmias, glaucoma, essential tremor, performance anxiety, migraine prophylaxis

    Side Effects: CH, bradycardia, AV block, bronchoconstriction, fatigue, sleep disturbance, depression, impair peripheral circulation (b2 receptors), sexual dysfunction in males, increased risk of hypoglycemic episodes in diabetes, increase risk of sudden death and exacerbation of angina pectoris with discontinued use

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