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Clinical pharmacy 2024/2025                            Level 3 Pharm D                             Pharmacology 1 (PO 502)

                                               1- Sympatholytics



                                           α-adrenoceptor blockers


           Classification                                     Pharmacological actions of α-blockers
           • Reversible non-selective α  1 & α  2          1.   BP by blocking of α-receptors.
            blockers ➔ Phentolamine.                       2.  Prevent pressor effects of α-agonists

           • Irreversible nonselective 1 blocker          3.  Reverse the action of E (E reversal).
            ➔ Phenoxybenzamine.

           • Selective α 1 blocker ➔ Prazosin.
           • Selective α 2 blockers ➔ Yohimbine

                           Uses of α-blockers                        Side effects of α-blockers:
           •  Essential hypertension & peripheral  ➢  Hypotension, tachycardia due to
              vascular diseases (e.g. CHF)                 1-  Normal reflex mechanism

           •  Pheochromocytoma (needs α & β-               2-   Non-selective block α 1& α  2➔B.P ➔
              blocker)                                        E which act on β1 (inotropic

           •  Bladder neck obstruction.                       chronotropic), β2 β3
                                                           ➢  Nasal congestion due to V. D

                      2- Phenoxybenzamine                            3- Phentolamine (Regitine)

               Irreversible nonselective α-blocker                       nonselective α- blocker

            delayed onset & long duration of                 Short acting α- receptors blocker.
              action.                                            (hypotension, tachycardia)

            Inhibits reuptake of NE (reuptake II).   Block  2 ➔ Epi, NE ➔ act on β1 (as
            Dirty drug: Block histamine (H 1),                  1,2 are blocked)

              muscarinic receptor of Ach &                    direct vasodilator & cardiac inotropic
              serotonin receptors, block reuptake                actions.
            Used previously (no other choice                 Stimulates muscarinic, H1 & H2
              available)                                         receptors.

           ✓  ttt. of pheochromocytoma.                      ✓  Diagnosis of pheochromocytoma (as

           ✓  In bladder neck obstruction.                       it is short acting).
                                                             ✓  ttt. Of hypertensive crises.















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