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

                                   8- α/β Adrenoreceptors blocking gents


            ➢  Labetalol and carvedilol  ➔ block α1, β1, and β2 receptors.
            ➢  Carvedilol ➔ effective antihypertensive, is mainly used in the treatment of heart
               failure.

            ➢  Carvedilol& metoprolol [selective β1 antagonist]➔ ↓ morbidity and mortality
               associated with heart failure.
                                    9- Centrally acting adrenergic drugs



                                          Clonidine                               α-methyldopa
                           α2- agonist (auto regulatory receptor)  α2-agonist ➔converted to methyl

                           ➔ ↓central adrenergic outflow ➔              norepinephrine centrally to
              MOA
                           ↓firing rate of sympathetic nerves &         diminish adrenergic outflow from
                           ↓ amount of NE release.                      the CNS.


                           ➢  Primarily for the treatment of
                              resistant hypertension  ➔  not           ➢  treating hypertensive patients
                              responded adequately to treatment            with renal insufficiency.

              Uses            with two or more drugs.                  ➢  hypertensive pregnant
                           ➢  Because it may cause sodium and              patients.
                              water retention, clonidine may be            (Almost reserved to this use) to

                              administrated in combination with            avoids Eclampsia
                              a diuretic.
                           ➢  Doesn’t decrease renal blood flow  ➢  ↓total peripheral resistance  ➔

                              or glomerular filtration➔ useful             ↓blood pressure.
             Action/
                              in the treatment of hypertension  ➢  Cardiac output is not decreased,
          Advantages          complicated by renal disease                 and blood flow to vital organs

                                                                           (kidney) is not diminished  ➔
                                                                           so used in renal failure

                             Mild →  sedation, dry mouth, and
               ADR                                                            sedation and drowsiness.
                                         constipation.

                           Rebound hypertension ➔ if drug

                           stopped suddenly ➔ NE ↑ to high
                           values and may cause cardiac arrest.
            Caution        occurs following abrupt withdrawal

                           of clonidine. [The drug should,
                           therefore, be withdrawn slowly if the
                           clinician wishes to change agents]





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