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					                PHARMACOLOGY 4Th Year                                                             ‫بسم هللا الرحمن الرحيم الفتاح العليم‬                                                     Dr.JKR
Category            Name            R Characters                                        Actions                                          Clinical Use                  Adverse A                    Notes / Drug Interaction
Cholinergic Agonist
                                      Quaternary Amine, Not pass                        ↓ H.rate & output, ↓ BP, ↑ Salivary              Not used clinically           __                           __
                                    M BBB, No therapeutic use duo to                    intestinal & motility of gut,↑ bronchiolar
                    1
                      Acetylcholine & multiplicity action & rapid in                    secretion, ↑tone of detrusor urinae,
                                    N activation by cholinesterase.                     stimulate ciliary M fore near vision,
                                                                                        Miosis
                                                                                                                                         1
                                                   Related structurally to Ach, Not     ↑ gut motility, ↑ tone of detrusor urinae          Stimulate atonic bladder    Sweating, salivation,        __
                          2                        hydrolyzed by cholinesterase,        with relaxation of tigone + sphincter           in post partum + post         flushing, ↓BP. Nausea,
                              Bethanechol     M
                                                   stimulate M mostly in                expulsion of urine.                              operative non obstructive     Abd. Pain, Diarrhea,
     Directly
                                                   GIT+Bladder                                                                           urinary retention             bronchospasm
      acting                                       Not or poorly hydrolyzed by          Has an actions on heart & GIT, release of        1
                                                                                                                                           Eye drops  Miosis         Slight or no side effect     1
                                                                                                                                                                                                     Folloing atropine ↑ BP
                              3               M&
                               Carbachol       N
                                                   cholinesterase                       EP from adrenal medulla by nicotinic             treatment of glaucoma
                                                                                        action
                                                   Tertiary amine, alkaloid, Pass       Rapid miosis, contraction ciliary body           1
                                                                                                                                           Emergency treatment of      Enter BBB  CNS              __
                                                   BBB                                                                                   both narrow+wide angle        distubances
                          4                                                                                                              glaucoma, 2with
                              Pilocarpine     M
                                                                                                                                         xerostomia (sjogren
                                                                                                                                         sumdrome) as it cause
                                                                                                                                         salivation
                                                                                                                                         1
                                                   Carbamate, Tertiary amine,                                                              Bladder + GIT atony,        Rarely: CNS                  __
                      1                                                                                                                  2
                       Physostigmine               alkaloid, Pass BBB, nicotinic                                                           Eye drops for glaucoma,     disturbance
                                                                                                                                         3
                                                   effect on NMJ,                                                                          Over dose of atropine       Bradycardia, fall in CO
    Reversible                                     Carbamate, Synthetic Quaternary      Duo to accumulation of Ach  muscle              1
                                                                                                                                           antidote to Tubocurarine,   Generalize cholinergic       __
                                                                                                                                         2
                          2                   M    Amine, Not pass BBB, greater         stimulation then paralysis,                         Bladder + GIT atony,       stimulation
                              Neostigmine                                                                                                3
 Indirect-acting                              &    effect on skeletal M than                                                               Myasthenia gravis(MG)
                                              N    Physostigmine.
(anticholinestrase)   3
                          Pyridostigmin                                                 Longer than Neostigmine                          Chronic managment of               //        //            __
                                e                                                                                                        MG
                      4                            Quaternary Amine                     Similar to Neostigmine but more rapidly                                        Excess drug may cause        Atropine is the antidote
                          Edrophonium                                                                                                    Diagnosis of MG
                                                                                        absorbed and short duration(10-20)min                                          cholinergic crisis
    Irreversible                                   Covalently bind,                     Generalized cholinergic stimulation,             Ointment for chronic          See its action.              Atropine is the antidote
                          Isoflurophate       M&
  Indirect-acting
                                               N
                                                   organophosphate, chemical war        paralysis of motor function(difficult            treatment of opened angle                                  peripherally + centrally
(anticholinestrase)           (DFP)
                                                   fare or nerve gas.                   breathing), intense miosis, convulsions          glaucoma last for 1 week
                                                   Synthetic Pyridinium compound,       Reactivation inhabited                           Given before aging of
  Reactivation of         Pralidoxime
acetylcholinestrase
                                                   not pass BBB duo to charged          acetylcholinestrase, reverse effect of           alkylated enzyme occurs
                            (PAM)
                                                   group                                organphosphat except CNS

Cholinergic Antagonist
                                                                                                                                         1
                                                   Belladonna alkaloid,Tertiary         Mydriasis, cycloplegia, ↓GIT activity              Mydriasis + cyclopegia,     Dry mouth, blurred           Pirenzepine M1 antagonist
                                                   amine, pass BBB, competitively       (antispasmodic effect), HCL secretion not        Contraindicated with          vision, sandy eyes,          ↓ gastric secretion
                                                   bind, action last 4 hr but in eye    affected, ↓ bladder motility(enuresis),          narrow glaucoma, 2GIT         tachycardia,
                                                   for several days, readily absorbed   tachycardia at high dose, at toxic dose          antispasmodic,                constipation, CNS
                                                                                                                                         3
                                  1                from GIT, partially metabolized      dilate coetaneous vasculature, block               organophosphate antidote    effect:
 AntiMuscarinc                     Atropine   M
                                                   by liver, eliminated in urine        salivary sweat lacrimal secretion ↑             peripherally + centrally,     confusion,hallucination,
                                                                                                                                         4
                                                                                        temperature                                        antisecretory               delirium,collapse of
                                                                                                                                         preanasethetic before         CVS + respiratory
                                                                                                                                         surg.                         system  death.
                                                  Belladonna alkaloid,Tertiary          Peripherally like atropine, centrally        1
                                                                                                                                       antimotion sickness
                          2                                                                                                           2
                           Scopolamine            amine, pass BBB,                      sedation not stimulation like atropine,        preanesthetic.
                            (Hyoscine)                                                  block short term memory, Mydriasis,
  AntiMuscarinc
                                                                                        cycloplegia
                          3                       Quaternary Amine, not pass BBB,                                                     1
                                                                                                                                       Bronchial asthma,                                     Benztropine inter CNS 
                              Ipratropium                                                                                             2
                                                  by inhalation                                                                        COPD                                                  treat Parkinsonism
Ganglionic Blocker                                Component of tobacco, depending       Stimulatory:↑ BP, tachycardia,↑               __
(Act on nicotinic R            1                  on the dose it first stimulate then   peristalsis, ↑secretion.
  but not at NMJ)               Nicotine
                                                  paralyses all ganglia cuz it          At high dose: ↓ BP, ↓ peristalsis,
    * all are non
                                                  depolarize the ganglia,               ↓secretions.
    depolarizing
    competitive                                                                                                                       Emergency treatment of
                                            N                                                                                         HTN caused by
 antagonist except                                Short acting, competitive, non
                      2
    for Nicotine       Trimethaphan                                                                                                   pulmonary edema or
                                                  depolarizing,
   * non selective                                                                                                                    dissecting aortic aneurysm
 between Symp. &                                                                                                                      by IV infusion
     Parasymp.        3
      Ganglia.            Mecamylamin             Orally, active for 10 hr
  Neuromuscular
      Blocking
                                                  Non depolarizing, competitive,        At low dose: on nicotinic prevent Ach         Adjuvant drug in             Respiratory paralysis,    Overcame by
                                                  alkaloid,Tubocurarine , IV, Not       bind competitively  inhibit muscle           anesthesia during surgery    histamine release,        anticholinestrase,
                                                  pass BBB , not metabolize so          contraction, Overcame by ↑ Ach by             to relax skeletal muscle     hypotension               Halothane to potentiate
                               1
                                   Curare         terminated by redistribution          anticholinestrase.                                                                                   the block, aminoglycoside
                                                                                        At high dose: block ion channels of the                                                              antibiotic, Ca+ channel
  A- antagonist                                                                         end plate weakening of neuromuscular                                                                blocker.
 Non depolarizing                           N
                                                                                        transmission.
   competitive
                          2                 at    Spontaneously degraded in                                                           In mechanical ventilation
                              Atracurium
                                                  plasma                                                                              & short surgical procedure
                          3                 the
                        Mivacurium                Short acting hydrolyzed by cholinesterase
                          4
                        Rocuronium                                                                                                    In tracheal intubation
                      5                     NMJ
                        Pancuronium                                                     Increase HR by vagolytic action
                                                  - Dose not block ganglia or           (phase1)cause opening of Na channel of        With tracheal intubation     Malignant
                                                  produce histamine like                N receptor  depolarization                  And with ECT                 hyperthermia, paralysis
    B- agonist
   depolarizing
                      Succinylcholin              Tubocurarine                          fasciculation, (phase2) gradual                                            of diaphragm and apnea
                                                  - short duration cuz broken down      repolarization  resistance to                                             if plasma cholinesrase
                                                  by plasma cholinesrase , used IV      depolarization  Flaccid paralysis                                         deficincy
                       Diazepam                   Act in CNS or in skeletal muscle      Diazepam, Baclofen, Tizanidine act                                                                   Gabapentin spasmolytic in
   C- drug for          Baclofen                  cell rather than NMJ                  centrally in spinal cord                                                                             pt with multiple sclerosis.
  chronic spasm        Tizanidine                                                       Dantrolene act in skeletal muscle cell
                       dantrolene
D- Drug for acute     Cyclobenzapri               Most are sedative act on brain                                                                                   Confusion,                Not effective with cerebral
 muscle spasm              ne                     stem or spinal cord, orally,                                                                                     hallucination,            palsy or spinal cord injury
Adrenergic Agonist
                                                                                                                                      1
                                                  Catecholamine, high potency,          α effect at high dose, β1effect at low dose     acute asthma,              CNS disturbance,          Enhanced CV response
                                                  rapid inactivation by COMT +          +ve inotropic & +ve chronotropic  β          2
                                                                                                                                        anaphylactic shock SC      anxiety, fear             with Cocaine, with
                                                  MAO, poor pass to CNS, not            constriction arterioles of skin mm and        type 1 hypersensitivity,     tension,headache.         hyperthyroidism
                              EP             α    orally but SC or IV or inhalation,    viscera  α                                   3
                                                                                                                                        open angle glaucoma, 4to   Tremor, cerebral
   Direct acting
                          (Adrenaline)       β                                          dilate vessel to liver & skeletal M β2       local anesthesia to          hemorrhage, cardiac
                                                                                        ↓ renal BF, net effect ↑ systolic BP &        prolongate the effect,       arrhythmias, pulmonary
                                                                                        slight ↓ diastolic BP lead to reflex                                       edema,
                                                                                        bradycardia, powerful bronchodilation- β2
                                                                                Hyperglycemia, ↑ glycogenolysis – relase
                                                                                of glucagons(β2), ↓ insulin(α2),lipolysis,
                                                                                Vasoconstriction, ↑ systolic & diastolic     In shock to rise BP                                       Atropine before NE 
                        NE
                                     α                                          BP, bradycardia duo to vagal stimulation                                                               tachycardia
                   (noradrenalin)
                                                                                of baroreceptor,
                                           Synthetic CA, inhalation or IV,      Intense +ve inotropic & chronotropic,        Stimulate the heart in        Like EP
                                    β1     not metabolized by MAO but by        dilate arterioles of SM↓ peripheral         emergency
                   Isoproterenol
                                    β2     COMT                                 resistance, ↓ mean BP & diastolic BP,
  Direct acting                                                                 Bronchodilation, hyperglycemia,
                                           Precursor of NE, naturally in CNS    α effect at high dose vasoconstriction,     Shock , CHF. ↑ BP             Nausea, HTN,
                                    α      in Basal ganglia, as                 β1effect at low dose +ve inotropic &                                      arrhythmia
                                    β      neurotransmitter & in the adrenal    chronotropic
                     Dopamine
                                    D1     medulla, IV                          D receptor in mesenteric & renal vascular
                                    D2                                          bed vasodilatation, D2 in presynaptic
                                                                                adrenergic neuron ↓ NE release
                                                                                ↑ CO with little change in HR & not ↑ O2                                                               Caution in use with atrial
                    Dobutamine      β1     Synthetic CA,                                                                     CHF
                                                                                consumption.                                                                                           fibrillation
                                           Not a CA, not substrate for          Vasoconstrictor  ↑ diastolic & systolic     1
                                                                                                                              nasal decongestant,          Large doses  HTN &
                   Phenylephrine    α1                                                                                       2
                                           COMT, lipid soluble pass BBB        BP, reflex Bradycardia,                       mydriasis, 3SVT,             cardiac irregularities.
                                                                                                                             In surgery to offset HTN
                   Methoxamine      α1     Like Phenylephrine                                                                produced by Halothane,
                                                                                                                             SVT
                                                                                Central inhibitory effect on sympathetic     Antihypertensive
                     Clonidine      α2
                                                                                vasomotor centers
                   Metaproterenol          Used orally or by inhalation                                                      - Bronchial asthma
                    Terbutaline                                                                                              - Terbutaline : reduce
                     Albuterol      β2                                                                                       uterine contraction in
                    Salbutamol                                                                                               premature labor
                    salmeterol
                                     α                                          Produces marked CNS stimulation, HTN,        In hyperkinetic children,
                   Amphetamine
                                     β                                          tachycardia,                                 narcolepsy, appetit control
 Indirect acting
                                           Inn fermented food,                                                               No uses                       Pt using MAO-inhibitor
                     Tyramine
                                                                                                                                                            Hypertensive crisis
                                           Alkaloid, not a CA, long duration,   ↑ sys & diastolic BP, tachycardia,           Prophylactic in chronic
                                     α
                    Ephedrine              orally, enter CNS,                   Bronchodilation, ↑ alertness, prevent        asthma, treat MG, nasal
  Mixed Action                       β
                                                                                sleep,                                       decongestant, raise BP
                    Metaraminol                                                 Action similar to NE                         Treatment of shock
Adrenergic Antagonist
                                           Orally active, long duration, bind   ↓ peripheral resistance, ↓ BP, reflex        -Not used in treat of HTN,    Postural hypotension,
                   Phenoxybenza            covalently irreversibly,             tachycardia, contribute to ↑ CO by block     - For pheochrmocytoma,        nasal stuffiness, nausea,
                                    α1,2
                       mine                                                     α2                                           - In chronic management       vomiting, tachycardia,
                                                                                                                             of tumor, - Raynaud's dis.    inhibition ejaculation
                   Phentolamine            Reversible, short action,                                                         Diagnosis of                  Arrhythmia, anginal
                                    α1,2
  α - Blockers       Tolazoline            competitive antagonist                                                            pheochrmocytoma               pain
                    Yohimbine       α2                                                                                       No uses
                     Prazocin              * Tamsulosin is amore potent         ↓ peripheral resistance, ↓ BP, cause         HTN, benign prostatic         1st dose phenomenon:
                     Terazocin             inhibitor of α1A , has minimal       minimal change in CO RBF GFR,                hyperplasia (Tamsulosin)      Postural hypotension,
                                    α1
                     Doxazocin             effect on BP, Doxazocin has                                                                                     fainting, nasal
                    Tamsulosin             longest action                                                                                                  stuffiness, dizziness
  β - Blockers      Propranolol     β1,2   Competitive,                         ↓ CO, -ve inotropic chronotropic,            HTN, glaucoma(↓               Bronchoconstruction,        Contraindicated in asthma,
                                                                                        bradycardia, ↓ O2 consumption,              secretion of aqueous          arrhythmia, metabolism       Cimetidine, furosemidine,
                                                                                        peripheral vasoconstriction, ↑ Na           humor), migraine, angina,     distybances, sexual          chlorpromazine potentiate
                                                                                        retention, ↓ glycogenolysis, ↓ glucagons    MI, hyperthyroidism,          impairment,                  the effect, phenytoin,
                                                                                        production, block action of Isoproterenol   arrhythmia, supra                                          rifampin,Phenobarbital 
                                                                                                                                    ventricular arrhythmia                                     ↑ its metabolism
                       Acebutolol                Esmolol very short action,                                                         IV in emergency for                                        B – blocker cause
                        Atenolol                                                                                                    arrhythmia                                                 symptomatic cardiac
                                         β1
                       Metoprolol                                                                                                                                                              depression
                        esmolol
                        Pindolol         α       Antagonist with partial agonist        Partial intrinsic sympathetic activity ,
                       Acebutolol        β                                              effective in HTN pt with bradycardia
                       Labetalol         α       Reversible B blocker with alpha-1                                                  Sever HTN                     Orthostatic hypotension
α & β - Blockers
                       carvedilol        β       block,                                                                                                           dizziness
  Drug affecting                                 Plant alkaloid, centrally and          Block Mg/ATP transport of biogenic          HTN
neurotramsmitter       Reserpine                 peripherally action                    amines from cytoplasm to storage vesicle
release or up take
                                                 Only preipherally                      Inhibit response to adrenergic nerve        In sever HTN,                 Orthostatic
                                                                                        syimulation or to indirectly acting                                       hypotension, sexual
                      Guanethidine
                                                                                        sympathomimetic drugs by block release                                    impairment,
                                                                                        of stored NE.
                                                                                        Inhibit reuptake of NE into neuron         Local anesthetic, CNS         Abuse  addiction
                        Cacaine
                                                                                        enhanced sympathetic activity               stimulant



    Glaucoma treatment                      Carbachol                              Pilocarpine                       Not pass BBB                   Acetylecholine                     Bethanechol
                                       Isoflurophate (wide)                          Timolol                                                         Neostigmine                        Carbachol
                                    EP( wide)     physosyigmine                    propranolol                                                      Edrophonium                Ipratropium         CA

          Pass BBB                           Pilocarpine                      Physostigmine                             In HTN                      trimethophane                           Colinidin
                                              Atropine                         Scopolamine                                                       Selective a1 blocker                       B blocker
                                            Non CA                              Ephedrine
                                          Phenylephrine                        amphetamine                               shock                           NE                             Phenylephrine
                                                                                                                                                      ephedrine                           dopamine
          In asthma                    EP          ipratropine                 Isoprterenole
                                         Metaproterenol                 Salmeterol       Terbutaline                      SVT              Phenylephrine        propronalol             Methaxamine
                                          Salbutamol                    Albuterol         ephedrine

             CHF                              dobutamine                Dopamine            carvidilol

				
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posted:8/25/2012
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