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Alpha Adrenergic AntagonistAka: Prazosin, Minipress, Terazosin, Hytrin, Doxazosin, Cardura, Tamsulosin, Flomax

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  1. Indications
    1. Benign Prostatic Hypertrophy
    2. Hypertension (not Tamsulosin)
  2. Mechanism: General
    1. See Alpha Adrenergic Receptor (Alpha-1 antagonist)
  3. Mechanism: Benign Prostatic Hypertrophy
    1. Preparations used in Benign Prostatic Hypertrophy
      1. Terazosin (Hytrin)
      2. Doxazosin (Cardura)
      3. Tamsulosin (Flomax)
      4. Prazosin (Minipress)
    2. Rapid relaxation of smooth muscle tone
      1. Bladder neck
      2. Prostate Capsule
      3. Prostatic Urethra
    3. Relieves symptoms of urinary obstruction
      1. May see full effect within 2 weeks
    4. Does not effect size of prostate (unlike Proscar)
  4. Preparations
    1. Prazosin (Minipress)
      1. Dose: 1 mg PO bid-tid (Maximum 40 mg/day)
      2. Less expensive but not available for once daily dose
    2. Terazosin (Hytrin)
      1. Dose: 1 mg PO qhs (Maximum 20 mg/day)
    3. Doxazosin (Cardura)
      1. Dose: 1 mg PO qd (Maximum 16 mg/day)
    4. Phenoxybenzamine (Dibenzyline)
      1. Dose: 10 mg PO bid (Maximum 120 mg/day)
    5. Tamsulosin (Flomax)
      1. More expensive than other agents
      2. Dose 0.4 mg PO qd (maximum 0.8 mg/day)
      3. Highly selective alpha-1a blocker
        1. Does not effect Blood Pressure
        2. May be more effective in BPH than other agents
  5. Combination Alpha-Beta Antagonist (Labetalol or Trandate)
    1. Oral: 100 mg PO bid (Maximum: 2400 mg/day)
    2. Intravenous: 20 mg IV q10 minutes (Maximum: 200 mg)
  6. Adverse effects (Incidence: 7 to 9%)
    1. Dose at bed and slowly titrate to reduce side effects
    2. Cardiovascular adverse effects (not Tamsulosin)
      1. Dizziness
      2. Postural Hypotension
    3. Other adverse effects
      1. Fatigue
      2. Asthenia
  7. Precautions
    1. Avoid using as monotherapy for Hypertension
      1. Higher risk of CVA and CHF compared with other agents
      2. (2000) JAMA 283:1967
  8. References
    1. (1994) Med Lett Drugs Ther 36:15
    2. (1997) Med Lett Drugs Ther 39:1011
    3. Lee (2000) Ann Pharmacother 34:188
    4. Aldridge (1996) Lancet 348:602

Prazosin (C0032912)

Definition (MSH)A selective adrenergic alpha-1 antagonist used in the treatment of heart failure, hypertension, pheochromocytoma, Raynaud's syndrome, prostatic hypertrophy, and urinary retention.
Definition (CSP)1-(4-amino-6,7-dimethoxy- 2-quinazolinyl) -4-(2-furoyl) piperazine.
Definition (NCI)A synthetic piperazine derivative and an alpha-1 adrenergic receptor inhibitor used primarily as an anti-hypertensive. Prazosin's effects are most pronounced in the large resistance vessels (i.e. arterioles) resulting in a decrease in the total systemic vascular resistance (SVR) without a rebound or reflex tachycardia. To a lesser extent, this agent also decreases the tone of the bladder sphincter, thereby allowing the opening of the bladder into the urethra, by which relieve urinary conditions associated with benign prostatic hypertrophy.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD011224
EnglishFurazosin, Prazosin, PRAZOSIN PREPARATION
Spanishfurazosin, furazosina, prazosin, prazosina
Parent ConceptsQuinazolines (C0034407), Antihypertensive Agents (C0003364), piperazine (C0031957), Adrenergic alpha-Antagonists (C0001641), [CV150] ALPHA-BLOCKERS/RELATED (C0973514), Alpha 1 adrenergic blocking agent (C0304512), Erroneous concept (C1274015)
SourcesAOD, CSP, LCH, LNC, MSH, MTHFDA, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


terazosine (C0076107)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC041226
EnglishTerazosin, TERAZOSIN PREPARATION, terazosine
Spanishterazosina
Parent ConceptsAdrenergic alpha-Antagonists (C0001641), Prazosin (C0032912), [CV150] ALPHA-BLOCKERS/RELATED (C0973514), Alpha 1 adrenergic blocking agent (C0304512), Drug allergen (C1320237), Duplicate concept (C1274013)
SourcesMSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Doxazosin (C0114873)

Definition (MSH)A selective alpha-1-adrenergic blocker that lowers serum CHOLESTEROL. It is also effective in the treatment of HYPERTENSION.
Definition (NCI)A quinazoline with antihypertensive and antineoplastic properties. Doxazosin is an alpha-adrenergic antagonist that selectively inhibits alpha-1 adrenergic receptors. Blockages of the alpha-1 adrenergic action on the vascular smooth muscles lead to a decrease in vascular resistance and antihypertensive activity. This agent also shows high affinity to alpha-1c adrenoceptor, the predominant functional type in the prostate, which may partially attribute to its effect in treatment of benign prostatic hyperplasia. Furthermore, doxazosin induces apoptosis in prostate cancer cells mediated through inhibition of protein kinase B (PKB)/Akt-signaling death receptor regulatory pathway.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD017292
EnglishDoxazosin, DOXAZOSIN PREPARATION
Spanishdoxazosina
Parent ConceptsPrazosin (C0032912), Adrenergic alpha-Antagonists (C0001641), Vasodilator Agents (C0042402), [CV150] ALPHA-BLOCKERS/RELATED (C0973514), Quinazolines (C0034407), Alpha 1 adrenergic blocking agent (C0304512)
SourcesCSP, MSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Minipress (C0242447)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD011224
EnglishMinipress
SourcesCSP, MSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


tamsulosin (C0257343)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC088482
Englishtamsulosin, TAMSULOSIN PREPARATION
Spanishtamsulosina
Parent ConceptsSulfonamides (C0038760), [GU900] GENITOURINARY AGENTS, OTHER (C0973562), Alpha 1 adrenergic blocking agent (C0304512), Drug allergen (C1320237), Adrenergic alpha-Antagonists (C0001641)
SourcesMSH, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Hytrin (C0591628)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC041226
EnglishAbbott brand of terazosine hydrochloride, Deflox, Flotrin, Heitrin, Hytrin, Hytrin BPH, Hytrine
SourcesMSH, MTH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Flomax (C0662903)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC088482
EnglishFlomax
SourcesMSH, NCI, PDQ, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Cardura (C0678136)

Definition (MSH)Trade name in United States.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD017292
EnglishAstraZeneca Brand of Doxazosin Mesylate, Cardular, Cardura, Carduran, Diblocin, Pfizer Brand of Doxazosin Mesylate, Zoxan
SourcesCSP, MSH, MTH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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