Pharmacology Drug Chart

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1 Pharmacology Drug Chart Cholinergic Agonists Acetylcholine Muscarinic HR, CO and BP Salivary Secretions Secretions and Motility in the GIT Bronchiolar Secretions Miosis (Constriction of the Pupil) Pharmacology Drug Chart Page 1 Bethanechol Carbachol Muscarinic Muscarinic Stimulates the detrusor while relaxing the trigone and sphincter causing urination in Nonobstructive retention i.e. postoperative and postpartum Similar to Bethanechol to treat urinary retention Used on the Eye to cause Miosis Intraocular Pressure to treat Glaucoma Sweating, Salivation, Flushing, BP, Nausea, Abdominal Pain, Diarrhea, and Bronchospasam When used to treat Glaucoma there are little to no side effects b/c of direct administration Pilocarpine Muscarinic Miosis Intraocular Pressure in BOTH Narrow and Wide angle Glaucoma Can enter the brain and cause CNS disturbances Sweating Salivation Anticholinesterases - Irreversible Covalently bonds to Chronic treatment of Open-angle Glaucoma Death Organophosphates AChase

2 Pharmacology Drug Chart Page 2 Anticholinesterases - Reversible Competitive Inhibitor Intestinal Motility Bradycardia of AChase Bladder Motility Can enter the CNS and high doses may cause Physostigmine Miosis Intraocular Pressure Used to treat an overdose of Atropine convulsions Neostigmine Competitive Inhibitor of AChase Intestinal Motility Bladder Motility Antidote for Tubocurarine Treatment of Myasthenia Gravis Sweating, Salivation, Flushing, BP, Nausea, Abdominal Pain, Diarrhea, and Bronchospasam Cholinergic Antagonists Non-specific Muscarinic Blocker via Competitive Binding Mydriasis (Dilation of the Pupil) Relaxes the GIT Antispasmodic activity in the Bladder Treatment of Organophosphate overdose by Dry Mouth Blurred Vision Tachycardia Constipation Atropine blocking the effects of excess ACh caused by Anti-AChase Blocks secretions of the upper and lower respiratory tract Intraocular Pressure (Bad for Glaucoma) Enters the CNS to cause Confusion, Hallucinations, Depression and collapse of the Circulatory and Respiratory systems

3 Pharmacology Drug Chart Page 3 Ganglionic and Neuromuscular Blockers Nicotine Low Dose - Ganglionic stimulation by depolarization High Dose - Ganglionic blockade Sympathetic Stimulation followed by paralysis of the ganglia Irritability and Tremors Intestinal Cramps and Diarrhea HR BP Rate of Metabolism of other drugs - Induction Hexamethonium (Trimethaphan) Competitive Nicotinic Ganglionic Blocker Used for the emergency lowering of BP Nondepolarizing NM Low Dose - Nicotinic Receptor and Histamine Release Blocker competitively blocks the binding of ACh Ganglionic Blockade Tubocurarine High Dose - blocks the Ion Channels of the End Plate BP Used to relax skeletal muscle during surgery Succinylcholine Depolarizing NM Blocker Rapid endothelial intubations Hyperthermia Apnea due to the paralysis of the Diaphragm

4 Direct Acting Adrenergic Agonists Low Dose β Med Dose D High Dose α ACTIONS Positive Inotropic β1 Positive Chronotropic β1 CO TPR Vasoconstriction in Skin and Viscera α1 Vasodilation in Liver and Skeletal Muscle β2 Renal blood flow Systolic Pressure CNS Disturbances Hemorrhage Cardiac Arrhythmias Pulmonary Edema Diastolic Pressure Epinephrine - Bronchodilation β2 FIGHT OR FLIGHT Glycogenolysis in Liver β2 Release of Glucagon β2 Release of Insulin α2 Lipolysis - β1 Receptors in Adipose Tissue THERAPEUTIC USES Intraocular Pressure ( Aqueous Humor) Used to treat Anaphylactic Shock Used to treat acute Asthma Pharmacology Drug Chart Page 4 Norepinephrine Mostly α1, α2 are for Negative Feedback β1 TPR BP Reflex Bradycardia

5 β1 and β2 Positive Inotropic CNS Disturbances Pharmacology Drug Chart Page 5 Isoproterenol / Isoprenaline Decreased Uptake Positive Chronotropic Vasodilation of Skeletal Muscle Bronchodilation Hemorrhage Cardiac Arrhythmias Pulmonary Edema High Dose α TPR Sympathetic Stimulation Med Dose β CO Nausea Dopamine Low Dose D TPR Drug of choice for shock because it Renal and Hypertension Arrhythmias Splanchnic blood flow Treatment of CHF β1 CO Use with caution in Atrial Fibrillation because the Dobutamine Treatment of CHF drug atrioventricular conduction Phenylephrine α1 and α2 but mostly Resistant to COMT α1 Vasoconstriction Systolic Pressure Diastolic Pressure Mydriasis Reflex Bradycardia Hypertensive Headache Cardiac Irregularities α2 BP due to its action on the CNS Clonidine Treatment for the withdrawal from Opiates and Benzodiazepines Salbutamol β2 Bronchodilation Treatment of Asthma Reflex Tachycardia α2 Agonist Sedation α-methyldopa TPR BP Drowsiness Organ Blood Flow is NOT Reduced

6 Indirect Acting Adrenergic Agonists α, β, CNS CNS stimulant in the treatment of children with BP ADD HR Amphetamine Also used in the treatment of Depression, Narcolepsy and Appetite Control Pharmacology Drug Chart Page 6 Mixed Acting Adrenergic Agonists α, β, CNS Resistant to COMT and MAO Treatment of Asthma BP HR Ephedrine Nasal Decongestant Fatigue Athletic Performance α Adrenergic Antagonists Phenoxybenzamine α1 and α2 Irreversible and Noncompetitive Treatment of Pheochromocytoma - a catecholamine secreting tumor Postural Hypotension Epinephrine Reversal Nasal Congestion Nausea Vomiting May induce Tachycardia Inhibits Ejaculation

7 α1 and α2 Used in the diagnosis of Pheochromocytoma Postural Hypotension Pharmacology Drug Chart Page 7 Competitive Tachycardia Phentolamine Cardiac Stimulation Epinephrine Reversal Anginal Pain Arrhythmias α1 Competitive First Dose Effect Syncope TPR Postural Hypotension Prazosin Alternative to surgery in benign Prostatic Hypertrophy thus improving urine flow Lack of Energy Nasal Congestion Headache β Adrenergic Antagonists Propranolol β1 and β2 Nonselective Intraocular Pressure Aqueous Humor Treatment of Migraine Curbing the effects of Hyperthyroidism Treatment of STABLE Angina (NOT ACUTE) Can aid in the prevention a Second MI Bronchoconstriction Arrhythmias Sexual Impairment (unclear as to why) Glycogenolysis Glucagon - Adverse of Insulin dependent diabetics β1 Selective May compromise respiratory activity in Cardioselective BP Asthmatics Atenolol Treatment of Angina Treatment of Atrial and Ventricular Arrhythmia Treatment of Tachycardia

8 α1 Antagonist Vasodilation Postural Hypotension α1 Pharmacology Drug Chart Page 8 β1 Antagonist BP Dizziness α1 Labetalol β2 Partial Agonist HR - Especially useful for patients with Asthma and Diabetics due to the β2 partial agonist effect Drugs Affecting Neurotransmitter Release Mg 2+ / ATP Dependent Transporter ACTION Blocks the Mg 2+ / ATP Dependent transporter from transporting Norepinephrine, Dopamine Causes the ultimate depletion of Norepinephrine in the adrenergic neuron Sympathetic function is greatly impaired Reserpine and Serotonin from the cytoplasm into the storage vesicles THERAPEUTIC USES May cause Bradycardia Mechanism 1 - Displaces Norepinephrine from Postural Hypotension storage vesicles Male sexual function interference Mechanism 2 - Blocks the release of stored Hypertensive Crisis in patients with Guanethidine Norepinephrine (Rarely Used) Pheochromocytoma due to a supersensitivity to Norepinephrine BP HR Na + / K + ATPase Inhibits reuptake 1 of Norepinephrine from the Causes the accumulation of Norepinephrine in Cocaine synaptic cleft by blocking Na/K ATPase the synaptic space Causes an enhancement of Sympathetic activity

9 Antiarrhythmic Drugs Binds to Open and Slows Phase 0 Depolarization May cause SA and AV Block Quinidine Inactive Na Channels Treatment of Atrial, AV, and Ventricular Asystole Class IA to Prevent Influx Arrhythmias May induce ventricular Tachycardia Na + Channel Blocker Pharmacology Drug Chart Page 9 Binds to Open and Shortens Phase 3 Repolarization Drowsiness Inactive Na Channels Suppresses arrhythmias caused by abnormal Slurred Speech to Prevent Influx automaticity within the cells Agitation Lidocaine Class IB Na + Channel Blocker Treatment of Ventricular Arrhythmias during MI Drug of choice for the emergency treatment of Cardiac Arrhythmias - Wide therapeutic to toxic ratio Confusion Convulsions Ventricular Arrhythmias Does not slow down conduction therefore it is not useful for AV junction arrhythmias Binds to Open and Markedly Slows Phase 0 Depolarization Negative Inotropic Flecainide Inactive Na Channels Treatment of Refractory Ventricular Can aggravate CHF Class IC to Prevent Influx Arrhythmias Ventricular Tachycardia Na + Channel Blocker Dizziness Blurred Vision

10 β1 and β2 Suppresses Phase 4 Depolarization Bronchoconstriction Pharmacology Drug Chart Page 10 Propranolol Class II β Adrenorecepter Blocker Nonselective camp causes Ca 2+ Influx in Cardiac Tissue which leads to CO HR Intraocular Pressure Aqueous Humor Treatment of Migraine Curbing the effects of Hyperthyroidism Treatment of STABLE Angina (NOT ACUTE) Treatment of arrhythmias caused by Arrhythmias Sexual Impairment (unclear as to why) Glycogenolysis Glucagon sympathetic activity Can aid in the prevention of a Second MI Binds to K Channels Prolongs Phase 3 Repolarization Interstitial Pulmonary Fibrosis to Diminish Outward Treatment of severe Supraventricular and GI Intolerance Amiodarone Class III K + Channel Blocker Current During Repolarization Ventricular Tachycardia Has Class I, II, III, IV Effects Hyper or Hypothyroidism Liver Toxicity Neuropathy Muscle Weakness Blue Skin (Iodine accumulation) Binds to Voltage Shortens Action Potential Negative Inotropic Gated Ca Channels Greater effect on the heart than on vascular BP due to peripheral vasodilation Verapamil Class IV Ca 2+ Channel Blocker to Decrease the Inward Current smooth muscle Treatment of Atrial Dysrhythmias Treatment of Reentrant Supraventricular Tachycardia Reduction in Atrial Flutter

11 Binds to Voltage Shortens Action Potential Negative Inotropic Pharmacology Drug Chart Page 11 Gated Ca Channels Greater effect on the heart than on vascular BP due to peripheral vasodilation Diltiazem Class IV Ca 2+ Channel Blocker to Decrease the Inward Current smooth muscle Treatment of Atrial Dysrhythmias Treatment of Reentrant Supraventricular Tachycardia Reduction in Atrial Flutter Blocks Na/K Shortens the refractory period in both the atria Can cause Ectopic ventricular beats Channels and and the ventricles while prolonging the effective Ventricular Tachycardia or Fibrillation Digoxin Reverses Ca/Na Antiport to refractory period and decreasing the conduction velocity Intracellular Ca Inhibits camp Slows AV Nodal Conduction Flushing Adenosine Dependent Ca and K Conduction Treatment of Supraventricular Tachycardia Shortness of Breath AV Block (Hyperpolarization) Mg 2+ Unknown Treatment of Digitalis Induced Arrhythmias Treatment of Ventricular Tachycardia

12 Pharmacology Drug Chart Page 12 Cardiac Glycosides Reversibly Binds with Digoxin is used in the treatment of severe left Progressively more severe Dysrhythmia the Na/K ATPase ventricular systolic dysfunction Supraventricular Tachycardia Positive Inotropic - improved circulation leads to Ventricular Fibrillation TPR and eventually HR Negative Chronotropic Complete Heart Block Small therapeutic level before Digitalis Toxicity - Digitalis Digoxin Digitoxin Ca overload together with diuretics Hyperkalemia Anorexia, Nausea and Vomiting Headache, Fatigue, Confusion, Blurred Vision, Alteration of Color Perception and Haloes Phosphodiesterase Inhibitors Inhibits camp causes Ca2+ Influx in Cardiac Tissue Toxicity and Death Milrinone / Amnirone Phosphodiesterase which leads to CO Enzyme Vasodilation Treatment of CHF

13 Pharmacology Drug Chart Page 13 Antihypertensive Drugs Thiazide Diuretics Bendrofluazide Mechanism Unknown Water and Na Excretion BP TPR CO [Ca2+] in the Urine Induce Hypokalemia and Hyperuricemia Can induce Hyperglycemia Gout Diabetics Mellitus Loop Diuretics Propranolol β1 and β2 Nonselective Cause Renal Vascular Resistance and Renal Blood Flow [Ca2+] in the Urine Used on patients with poor renal function rather than the Thiazide Diuretics Intraocular Pressure Aqueous Humor Treatment of Migraine Curbing the effects of Hyperthyroidism Treatment of STABLE Angina (NOT ACUTE) Can aid in the prevention of a Second MI Bronchoconstriction Arrhythmias Sexual Impairment (unclear as to why) Glycogenolysis Glucagon Atenolol β1 Selective Cardioselective BP Treatment of Angina Treatment of Atrial and Ventricular Arrhythmia Treatment of Tachycardia May compromise respiratory activity in Asthmatics

14 α1 Antagonist Vasodilation Postural Hypotension α1 Pharmacology Drug Chart Page 14 β1 Antagonist BP Dizziness α1 Labetalol β2 Partial Agonist HR - Especially useful for patients with Asthma and Diabetics due to the β2 partial agonist effect Blocks the ACE Peripheral Vascular Resistance without Dry Cough due to a diminished rate of enzyme affecting CO, HR or Contractility Bradykinin Inactivation ACE Inhibitors Captapril Renal Damage Rashes Fever First Dose Effect Syncope Highly Selective Similar to ACE Inhibitors Improved of ACE Inhibitors Angiotensin II Antagonists: Losartan Angiotensin II Receptor Blocker (AT 1 Subtype) Vasodilation Blocks Aldosterone Secretion No Dry cough because Bradykinin is not affected Fetotoxic α1 Competitive First Dose Effect Syncope Prazosin TPR Alternative to surgery in benign Prostatic Hypertrophy thus improving urine flow Postural Hypotension Lack of Energy Nasal Congestion Headache

15 Binds to Ca Channels Shortens Action Potential Negative Inotropic Pharmacology Drug Chart Page 15 to Decrease the Greater effect on the heart than on vascular BP due to peripheral vasodilation Verapamil Class IV Ca 2+ Channel Blocker Inward Current smooth muscle Treatment of Atrial Dysrhythmias Treatment of Reentrant Supraventricular Tachycardia Reduction in Atrial Flutter Binds to Ca Channels Shortens Action Potential Negative Inotropic to Decrease the Greater effect on the heart than on vascular BP due to peripheral vasodilation Diltiazem Class IV Ca 2+ Channel Blocker Inward Current smooth muscle Treatment of Atrial Dysrhythmias Treatment of Reentrant Supraventricular Tachycardia Reduction in Atrial Flutter α2 Agonist BP due to its action on the CNS Clonidine Treatment for the withdrawal from Opiates and Benzodiazepines α2 Agonist Sedation α-methyldopa TPR BP Organ Blood Flow is NOT Reduced Drowsiness

16 Reserpine Mg 2+ / ATP Dependent Transporter ACTION Blocks the Mg 2+ / ATP Dependent transporter from transporting Norepinephrine, Dopamine and Serotonin from the cytoplasm into the storage vesicles THERAPEUTIC USES Pharmacology Drug Chart Page 16 Causes the ultimate depletion of Norepinephrine in the adrenergic neuron Sympathetic function is greatly impaired May cause Bradycardia Vasodilators Hydralizine Atrial Dilation TPR Tachycardia GI discomfort Hirsuitism Minoxidil Atrial Dilation TPR Tachycardia GI discomfort Hirsuitism K+ Sparing Diuretics Competes with Leads to Na Secretion and K Retention Hyperkalemia Spirolactene Aldosterone Receptors Weak Diuretic

17 Pharmacology Drug Chart Page 17 Autacoids Abortion With Alprostadil there is pain at the site of Prostaglandins Peptic Ulcers injection Inhibits the secretion of HCl in the stomach Erectile Dysfunction (Alprostadil) Histamine H 1 H 2 H 1 and H 2 Bronchial and Intestinal Smooth Muscle Contraction NO Production of Nasal and Bronchial Mucus Stimulates Itch and Pain and Sensory Nerve Endings Gastric HCl secretion Systemic BP Peripheral Resistance Positive Inotropic (H 1 and H 2 ) Positive Chronotropic (H 2 ) Capillary Permeability Vasodilation Triple Response - Wheal Formation, Reddening and Halo Respiratory Symptoms Lung Capacity Intestinal Cramps Diarrhea

18 Antihistamines H 1 Receptor Competitive Treatment of Allergic Conditions CANNOT treat Bronchial Asthma Sedation Dry Mouth H 1 Receptor Blockers Chlorpheniramine Motion Sickness and Nausea Treatment of Insomnia Drug Interactions (MAO Inhibitors) Overdose in Children Tremor Vertigo Pharmacology Drug Chart Page 18 H 2 Receptor Blockers Cimetidine H 2 Receptor Competitive Treatment of Peptic Ulcers Gastric HCl Secretion

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