Sheet1Pharmacology Drug ChartCholinergic AgonistsDrug NameReceptorTherapeutic UsesAdverse EffectsAcetylcholineMuscarinic HR, CO and BP Salivary Secretions Secretions and Motility in the GIT Bronchiolar SecretionsMiosis (Constriction of the Pupil)BethanecholMuscarinicStimulates the detrusor while relaxing the trigone and sphincter causing urination in Nonobstructive retention i.e. postoperative and postpartumSweating, Salivation, Flushing, BP, Nausea, Abdominal Pain, Diarrhea, and BronchospasamCarbacholMuscarinicSimilar to Bethanechol to treat urinary retentionUsed on the Eye to cause Miosis Intraocular Pressure to treat GlaucomaWhen used to treat Glaucoma there are little to no side effects b/c of direct administrationPilocarpineMuscarinicMiosis Intraocular Pressure in BOTH Narrow and Wide angle GlaucomaCan enter the brain and cause CNS disturbances Sweating SalivationAnticholinesterases - IrreversibleDrug NameReceptorTherapeutic UsesAdverse EffectsOrganophosphatesCovalently bonds to AChaseChronic treatment of Open-angle GlaucomaDeath LAnticholinesterases - ReversibleDrug NameReceptorTherapeutic UsesAdverse EffectsPhysostigmineCompetitive Inhibitor of AChase Intestinal Motility Bladder MotilityMiosis Intraocular PressureUsed to treat an overdose of AtropineBradycardiaCan enter the CNS and high doses may cause convulsionsNeostigmineCompetitive Inhibitor of AChase Intestinal Motility Bladder MotilityAntidote for TubocurarineTreatment of Myasthenia GravisSweating, Salivation, Flushing, BP, Nausea, Abdominal Pain, Diarrhea, and BronchospasamCholinergic AntagonistsDrug NameReceptorTherapeutic UsesAdverse EffectsAtropineNon-specific Muscarinic Blocker via Competitive BindingMydriasis (Dilation of the Pupil)Relaxes the GITAntispasmodic activity in the BladderTreatment of Organophosphate overdose by blocking the effects of excess ACh caused by Anti-AChase Blocks secretions of the upper and lower respiratory tractDry MouthBlurred VisionTachycardiaConstipation Intraocular Pressure (Bad for Glaucoma)Enters the CNS to cause Confusion, Hallucinations, Depression and collapse of the Circulatory and Respiratory systemsGanglionic and Neuromuscular BlockersDrug NameReceptorTherapeutic UsesAdverse EffectsNicotineLow Dose - Ganglionic stimulation by depolarizationHigh Dose - Ganglionic blockadeSympathetic Stimulation followed by paralysis of the gangliaIrritability and TremorsIntestinal Cramps and Diarrhea HR BP Rate of Metabolism of other drugs - InductionHexamethonium(Trimethaphan)Competitive Nicotinic Ganglionic BlockerUsed for the emergency lowering of BPTubocurarineNondepolarizing NM BlockerLow Dose - Nicotinic Receptor and competitively blocks the binding of AChHigh Dose - blocks the Ion Channels of the End PlateUsed to relax skeletal muscle during surgeryHistamine ReleaseGanglionic Blockade BPSuccinylcholineDepolarizing NM BlockerRapid endothelial intubationsHyperthermiaApnea due to the paralysis of the DiaphragmDirect Acting Adrenergic AgonistsDrug NameReceptorTherapeutic UsesAdverse EffectsEpinephrine - FIGHT OR FLIGHTLow Dose bMed Dose DHigh Dose aACTIONSPositive Inotropic b1Positive Chronotropic b1 CO TPRVasoconstriction in Skin and Viscera a1Vasodilation in Liver and Skeletal Muscle b2 Renal blood flow Systolic Pressure Diastolic PressureBronchodilation b2 Glycogenolysis in Liver b2 Release of Glucagon b2 Release of Insulin a2 Lipolysis - b1 Receptors in Adipose TissueTHERAPEUTIC USES Intraocular Pressure ( Aqueous Humor)Used to treat Anaphylactic ShockUsed to treat acute AsthmaCNS DisturbancesHemorrhageCardiac ArrhythmiasPulmonary EdemaNorepinephrineMostly a1,a2 are for Negative Feedbackb1 TPR BPReflex BradycardiaIsoproterenol / Isoprenalineb1 and b2Decreased UptakePositive InotropicPositive ChronotropicVasodilation of Skeletal MuscleBronchodilationCNS DisturbancesHemorrhageCardiac ArrhythmiasPulmonary EdemaDopamineHigh Dose aMed Dose bLow Dose D TPR CO TPRDrug of choice for shock because it Renal and Splanchnic blood flowTreatment of CHFSympathetic StimulationNauseaHypertensionArrhythmiasDobutamineb1 COTreatment of CHFUse with caution in Atrial Fibrillation because the drug atrioventricular conductionPhenylephrinea1 and a2 but mostly a1Resistant to COMTVasoconstriction Systolic Pressure Diastolic PressureMydriasisReflex BradycardiaHypertensive HeadacheCardiac IrregularitiesClonidinea2 BP due to its action on the CNSTreatment of HypertensionTreatment for the withdrawal from Opiates and BenzodiazepinesSalbutamolb2BronchodilationTreatment of AsthmaReflex Tachycardiaa-Methyldopaa2 AgonistTreatment of Hypertension TPR BPOrgan Blood Flow is NOT ReducedSedationDrowsinessIndirect Acting Adrenergic AgonistsDrug NameReceptorTherapeutic UsesAdverse EffectsAmphetaminea, b, CNSCNS stimulant in the treatment of children with ADDAlso used in the treatment of Depression, Narcolepsy and Appetite Control BP HRMixed Acting Adrenergic AgonistsDrug NameReceptorTherapeutic UsesAdverse EffectsEphedrinea, b, CNSResistant to COMT and MAOTreatment of AsthmaNasal Decongestant Fatigue Athletic Performance BP HRa Adrenergic AntagonistsDrug NameReceptorTherapeutic UsesAdverse EffectsPhenoxybenzaminea1 and a2Irreversible and NoncompetitiveTreatment of Pheochromocytoma - a catecholamine secreting tumorPostural HypotensionEpinephrine ReversalNasal CongestionNauseaVomitingMay induce TachycardiaInhibits EjaculationPhentolaminea1 and a2 CompetitiveUsed in the diagnosis of PheochromocytomaPostural HypotensionTachycardiaCardiac StimulationEpinephrine ReversalAnginal PainArrhythmiasPrazosina1 CompetitiveTreatment of Hypertension TPRAlternative to surgery in benign Prostatic Hypertrophy thus improving urine flowFirst Dose Effect SyncopePostural HypotensionLack of EnergyNasal CongestionHeadacheb Adrenergic AntagonistsDrug NameReceptorTherapeutic UsesAdverse EffectsPropranololb1 and b2Nonselective Intraocular Pressure Aqueous HumorTreatment of MigraineCurbing the effects of HyperthyroidismTreatment of STABLE Angina (NOT ACUTE)Can aid in the prevention a Second MIBronchoconstrictionArrhythmiasSexual Impairment (unclear as to why) Glycogenolysis Glucagon - Adverse of Insulin dependent diabeticsAtenololb1 SelectiveCardioselectiveTreatment of Hypertension BPTreatment of AnginaTreatment of Atrial and Ventricular ArrhythmiaTreatment of TachycardiaMay compromise respiratory activity in AsthmaticsLabetalola1 Antagonistb1 Antagonistb2 Partial AgonistVasodilation BP HRTreatment of Hypertension - Especially useful for patients with Asthma and Diabetics due to the b2 partial agonist effectPostural Hypotension a1Dizziness a1Drugs Affecting Neurotransmitter ReleaseDrug NameReceptorTherapeutic UsesAdverse EffectsReserpineMg2+ / ATP Dependent TransporterACTIONBlocks the Mg2+ / ATP Dependent transporter from transporting Norepinephrine, Dopamine and Serotonin from the cytoplasm into the storage vesiclesTHERAPEUTIC USESTreatment of HypertensionCauses the ultimate depletion of Norepinephrine in the adrenergic neuronSympathetic function is greatly impairedMay cause BradycardiaGuanethidineMechanism 1 - Displaces Norepinephrine from storage vesiclesMechanism 2 - Blocks the release of stored NorepinephrineTreatment of Hypertension (Rarely Used) BP HRPostural HypotensionMale sexual function interferenceHypertensive Crisis in patients with Pheochromocytoma due to a supersensitivity to NorepinephrineCocaineNa+ / K+ ATPaseInhibits reuptake 1 of Norepinephrine from the synaptic cleft by blocking Na/K ATPaseCauses the accumulation of Norepinephrine in the synaptic spaceCauses an enhancement of Sympathetic activityAntiarrhythmic DrugsDrug NameReceptorTherapeutic UsesAdverse EffectsQuinidine Class IA Na+ Channel BlockerBinds to Open and Inactive Na Channels to Prevent InfluxSlows Phase 0 DepolarizationTreatment of Atrial, AV, and Ventricular ArrhythmiasMay cause SA and AV BlockAsystoleMay induce ventricular TachycardiaLidocaine Class IB Na+ Channel BlockerBinds to Open and Inactive Na Channels to Prevent InfluxShortens Phase 3 RepolarizationSuppresses arrhythmias caused by abnormal automaticity within the cellsTreatment of Ventricular Arrhythmias during MIDrug of choice for the emergency treatment of Cardiac Arrhythmias - Wide therapeutic to toxic ratioDrowsinessSlurred SpeechAgitationConfusionConvulsionsVentricular ArrhythmiasDoes not slow down conduction therefore it is not useful for AV junction arrhythmiasFlecainide Class IC Na+ Channel BlockerBinds to Open and Inactive Na Channels to Prevent InfluxMarkedly Slows Phase 0 DepolarizationTreatment of Refractory Ventricular ArrhythmiasNegative InotropicCan aggravate CHFVentricular TachycardiaDizzinessBlurred VisionPropranolol Class II b Adrenorecepter Blocker REPEATb1 and b2NonselectiveSuppresses Phase 4 Depolarization cAMP causes Ca2+ Influx in Cardiac Tissue which leads to CO HR Intraocular Pressure Aqueous HumorTreatment of MigraineCurbing the effects of HyperthyroidismTreatment of STABLE Angina (NOT ACUTE)Treatment of arrhythmias caused by sympathetic activityCan aid in the prevention of a Second MIBronchoconstrictionArrhythmiasSexual Impairment (unclear as to why) Glycogenolysis GlucagonAmiodarone Class III K+ Channel BlockerBinds to K Channels to Diminish Outward Current During RepolarizationProlongs Phase 3 RepolarizationTreatment of severe Supraventricular and Ventricular TachycardiaHas Class I, II, III, IV EffectsInterstitial Pulmonary FibrosisGI IntoleranceHyper or HypothyroidismLiver ToxicityNeuropathyMuscle WeaknessBlue Skin (Iodine accumulation)Verapamil Class IV Ca2+ Channel BlockerBinds to Voltage Gated Ca Channels to Decrease the Inward CurrentShortens Action PotentialGreater effect on the heart than on vascular smooth muscleTreatment of Atrial DysrhythmiasTreatment of Reentrant Supraventricular TachycardiaReduction in Atrial FlutterTreatment of HypertensionNegative Inotropic BP due to peripheral vasodilationDiltiazem Class IV Ca2+ Channel BlockerBinds to Voltage Gated Ca Channels to Decrease the Inward CurrentShortens Action PotentialGreater effect on the heart than on vascular smooth muscleTreatment of Atrial DysrhythmiasTreatment of Reentrant Supraventricular TachycardiaReduction in Atrial FlutterTreatment of HypertensionNegative Inotropic BP due to peripheral vasodilationDigoxinBlocks Na/K Channels andReverses Ca/Na Antiport to Intracellular CaShortens the refractory period in both the atria and the ventricles while prolonging the effective refractory period and decreasing the conduction velocityCan cause Ectopic ventricular beatsVentricular Tachycardia or FibrillationAdenosineInhibits cAMP Dependent Ca and K Conduction (Hyperpolarization)Slows AV Nodal ConductionTreatment of Supraventricular TachycardiaFlushingShortness of BreathAV BlockMg2+UnknownTreatment of Digitalis Induced ArrhythmiasTreatment of Ventricular TachycardiaCardiac GlycosidesDrug NameReceptorTherapeutic UsesAdverse EffectsDigitalis Digoxin DigitoxinReversibly Binds with the Na/K ATPaseDigoxin is used in the treatment of severe left ventricular systolic dysfunctionPositive Inotropic - improved circulation leads to TPR and eventually HRNegative ChronotropicProgressively more severe DysrhythmiaSupraventricular TachycardiaVentricular FibrillationComplete Heart BlockSmall therapeutic level before Digitalis Toxicity - Ca overload together with diureticsHyperkalemiaAnorexia, Nausea and VomitingHeadache, Fatigue, Confusion, Blurred Vision, Alteration of Color Perception and HaloesPhosphodiesterase InhibitorsDrug NameReceptorTherapeutic UsesAdverse EffectsMilrinone / AmnironeInhibits Phosphodiesterase Enzyme cAMP causes Ca2+ Influx in Cardiac Tissue which leads to CO VasodilationTreatment of CHFToxicity and Death LAntihypertensive DrugsDrug NameReceptorTherapeutic UsesAdverse EffectsThiazide DiureticsBendrofluazideMechanism UnknownTreatment of Hypertension Water and Na Excretion BP TPR CO [Ca2+] in the UrineInduce Hypokalemia and HyperuricemiaCan induce HyperglycemiaGoutDiabetics MellitusLoop DiureticsCause Renal Vascular Resistance and Renal Blood Flow [Ca2+] in the Urine Used on patients with poor renal function rather than the Thiazide DiureticsPropranololREPEATb1 and b2Nonselective Intraocular Pressure Aqueous HumorTreatment of MigraineCurbing the effects of HyperthyroidismTreatment of STABLE Angina (NOT ACUTE)Can aid in the prevention of a Second MIBronchoconstrictionArrhythmiasSexual Impairment (unclear as to why) Glycogenolysis GlucagonAtenololREPEATb1 SelectiveCardioselectiveTreatment of Hypertension BPTreatment of AnginaTreatment of Atrial and Ventricular ArrhythmiaTreatment of TachycardiaMay compromise respiratory activity in AsthmaticsLabetalolREPEATa1 Antagonistb1 Antagonistb2 Partial AgonistVasodilation BP HRTreatment of Hypertension - Especially useful for patients with Asthma and Diabetics due to the b2 partial agonist effectPostural Hypotension a1Dizziness a1ACE InhibitorsCaptaprilBlocks the ACE enzyme Peripheral Vascular Resistance without affecting CO, HR or ContractilityTreatment of HypertensionDry Cough due to a diminished rate of Bradykinin InactivationRenal DamageRashesFeverFirst Dose Effect SyncopeAngiotensin IIAntagonists:LosartanHighly Selective Angiotensin II Receptor Blocker (AT1 Subtype)Similar to ACE InhibitorsVasodilationBlocks Aldosterone SecretionNo Dry cough because Bradykinin is not affectedImproved of ACE InhibitorsFetotoxicPrazosinREPEATa1 CompetitiveTreatment of Hypertension TPRAlternative to surgery in benign Prostatic Hypertrophy thus improving urine flowFirst Dose Effect SyncopePostural HypotensionLack of EnergyNasal CongestionHeadacheVerapamil Class IV Ca2+ Channel Blocker REPEATBinds to Ca Channels to Decrease the Inward CurrentShortens Action PotentialGreater effect on the heart than on vascular smooth muscleTreatment of Atrial DysrhythmiasTreatment of Reentrant Supraventricular TachycardiaReduction in Atrial FlutterTreatment of HypertensionNegative Inotropic BP due to peripheral vasodilationDiltiazem Class IV Ca2+ Channel Blocker REPEATBinds to Ca Channels to Decrease the Inward CurrentShortens Action PotentialGreater effect on the heart than on vascular smooth muscleTreatment of Atrial DysrhythmiasTreatment of Reentrant Supraventricular TachycardiaReduction in Atrial FlutterTreatment of HypertensionNegative Inotropic BP due to peripheral vasodilationClonidineREPEATa2 Agonist BP due to its action on the CNSTreatment of HypertensionTreatment for the withdrawal from Opiates and Benzodiazepinesa-MethyldopaREPEATa2 AgonistTreatment of Hypertension TPR BPOrgan Blood Flow is NOT ReducedSedationDrowsinessReserpineREPEATMg2+ / ATP Dependent TransporterACTIONBlocks the Mg2+ / ATP Dependent transporter from transporting Norepinephrine, Dopamine and Serotonin from the cytoplasm into the storage vesiclesTHERAPEUTIC USESTreatment of HypertensionCauses the ultimate depletion of Norepinephrine in the adrenergic neuronSympathetic function is greatly impairedMay cause BradycardiaVasodilatorsDrug NameReceptorTherapeutic UsesAdverse EffectsHydralizineAtrial Dilation TPRTreatment of HypertensionTachycardiaGI discomfortHirsuitismMinoxidilAtrial Dilation TPRTreatment of HypertensionTachycardiaGI discomfortHirsuitismK+ Sparing DiureticsDrug NameReceptorTherapeutic UsesAdverse EffectsSpirolacteneCompetes with Aldosterone ReceptorsLeads to Na Secretion and K RetentionWeak DiureticHyperkalemiaAutacoidsDrug NameReceptorTherapeutic UsesAdverse EffectsProstaglandinsAbortionPeptic UlcersInhibits the secretion of HCl in the stomachErectile Dysfunction (Alprostadil)With Alprostadil there is pain at the site of injectionHistamineH1

H2H1 and H2Bronchial and Intestinal Smooth Muscle Contraction NO Production of Nasal and Bronchial MucusStimulates Itch and Pain and Sensory Nerve Endings Gastric HCl secretion Systemic BP Peripheral ResistancePositive Inotropic (H1 and H2)Positive Chronotropic (H2)Capillary PermeabilityVasodilationTriple Response - Wheal Formation, Reddening and HaloRespiratory Symptoms Lung CapacityIntestinal CrampsDiarrheaAntihistaminesDrug NameReceptorTherapeutic UsesAdverse EffectsH1 Receptor BlockersChlorpheniramineH1 ReceptorCompetitiveTreatment of Allergic ConditionsCANNOT treat Bronchial AsthmaMotion Sickness and NauseaTreatment of InsomniaSedationDry MouthDrug Interactions (MAO Inhibitors)Overdose in ChildrenTremorVertigoH2 Receptor Blockers CimetidineH2 ReceptorCompetitiveTreatment of Peptic Ulcers Gastric HCl Secretion

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