DOC G PHARMACOLOGY LECTURE.pdf

PHARMACOLOGY PHARMACODYNAMICS PHARMACOKINETIC NEUROTRANSMITTERS ACTION OF THE DRUG  RESPONSE OF THE BODY TO The body’s c...

PHARMACOLOGY PHARMACODYNAMICS PHARMACOKINETIC NEUROTRANSMITTERS ACTION OF THE DRUG  RESPONSE OF THE BODY TO The body’s chemical TO THE BODY THE DRUG “messengers”  “LADME” Produced by nerves Body (Cells) drug binds into: Receptors Replace a missing substance (Insulin, L Liberation Acetylcholine (Ach) Cortisol, T3 & T4) Release of active ingredients Muscle contraction Increase cellular Memory activities (Epinephrine) A Absorption LACK: Alzheimer’s Disease Depress cellular Bloodstream EXCESS: Bipolar/Mania activities (Beta-Blockers, Oral Slowest absorption NERVES: Cholinergic CCB) IV Most rapid absorption time Nerves Interfere the growth of a SUBQ & IM Depends on blood foreign body (Antibiotics) perfusion at injection site Norepinephrine/ Epinephrine (NE/Epi) Drug Action through: D Distribution Adrenaline 1. Receptors Bring to target tissue Released during SNS 2. Enzymes Transportation of the medication stimulation 3. Pumps by bodily fluids to where it needs LACK: Depression 4. Chemical to go EXCESS: Mania Interaction NERVES: Adrenergic Nerves 5. Alternating M Metabolism Metabolic Dopamine (Dopa) If oral Liver detoxification Process Motor (makes the drug less active) Behavior The breakdown of the medication Drug-Receptor Interactions LACK: Parkinson’s FIRST-PASS EFFECT: The A. Agonist EXCESS: Schizophrenia effect of the drug is reduced as Stimulates a receptor site Treatment for Schizophrenia: only part of the drug is reduced e.g. Opioid agonist Anti- as only part of the drug reaches (Morphine) binds to the psychotic/Neuroleptics: systemic circulation, they are receptor. Typical: blocks dopa receptor LESS POWERFUL & will not Atypical: blocks dopa & 5Ht produce a full therapeutic effect. B. Competitive Antagonist receptor Blocks the receptor site E Excretion Blocks the action of the antagonist Serotonin 5-hydroxytryptamine The removal of the (5-HT) e.g. Opioid Antagonist unmetabolized medication from (Naloxone) Arousal, Sleep & the body. Motivation Flumazenil Most commonly done by kidneys (Benzodiazepine Overdose Behavior (urine) EXCESS: Schizophrenia Acetylcysteine GIT (poops) & Skin (sweat) (Acetaminophen Overdose) NERVES: Serotonergic nerves C. Non-Competitive Antagonist Gamma-aminobutyric acid Blocks the receptor site (GABA) Reduces action of agonist Inhibitory neurotransmitter e.g. Cephalosporin Used in seizure reduced by PPI NERVES: Gabaminergic nerves Drug-Enzyme Interactions e.g. Cholinesterase Inhibitors Breakdown Ach(“stigmines”) Chemical Interaction Antacid Interrupting Metabolic Processes Insulin  AUTONOMIC NERVOUS SYSTEM SYMPATHETIC NERVOUS SYSTEM PARASYMPATHETIC NERVOUS SYSTEM ADRENERGIC NERVOUS SYSTEM CHOLINERGIC NERVOUS SYSTEM Neurotransmitter: Neurotransmitter: Preganglionic: Acetylcholine (Ach) Preganglionic: Acetylcholine (Ach) Postganglionic: Norepinephrine Postganglionic: Acetylcholine (Ach) General Response FIGHT or FLIGHT REST and DIGEST Origin Thoracolumbar Craniosacral Preganglionic Short Long Neurotransmitter Acetylcholine (Ach) Acetylcholine (Ach) Postganglionic Long Short Neurotransmitter Norepinephrine Acetylcholine (Ach) Termination of Monoamine oxidase (MAO) Impulse Catechol-O-methyltransferase (COMT) Cholinesterase BODY’S RESPONSE Heart HR HR Contractility Contractility Bronchus Bronchodilation Bronchoconstriction Pupils Dilate Constrict (MYDRIASIS) (MIOSIS) GIT Constipation Diarrhea Urinary Bladder Retention of Urine Emptying of Urine Sphincter Contract Relax Detrusor Muscle Relax Contract Blood Vessels Vasoconstriction Vasodilation SYMPATHETIC NERVOUS SYSTEM PARASYMPATHETIC NERVOUS SYSTEM ADRENERGIC NERVOUS SYSTEM CHOLINERGIC NERVOUS SYSTEM Agonist = stimulate/activate Antagonist = block Mimetic = mimic, copy Lytic = block, destroy, dissolve AUTONOMIC NERVOUS SYSTEM DRUGS ADRENERGIC AGONIST | SYMPATHOMIMETIC Adrenergic Agonist Alpha Adrenergic Alpha-2 Beta-1 Adrenergic Beta-2 Adrenergic Agonist Agonist Adrenergic Agonist Agonist a. Epinephrine a. Midodrine a. Clonidine a. Dobutamine a. Albuterol/Salbutamol b. Dobutamine (Catapres) b. Terbutaline c. Dopamine b. Methyldopa c. Formoterol d. Norepinephrine (Aldomet) d. Salmeterol ADRENERGIC ANTAGONIST | SYMPATHOLYTIC Alpha and Beta Alpha Adrenergic Alpha-1 Adrenergic Beta-Adrenergic Beta-1 Specific Adrenergic Antagonist Antagonist Antagonist Adrenergic Antagonist Antagonist a. Carvediol a. Phentolamine b. Prazosin a. Propranolol a. Betaxolol b. Labetalol c. Doxazosin b. Timolol b. Esmolol d. Terazosin c. Atenolol e. Alfuzosin d. Metoprolol f. Tamsulosin e. Bisoprostol f. Acebutolol ATROPINE SULFATE Drug Class: Anticholinergic Drug used in pre-operative and patients with bradycardia Action: SNS Effect decreases secretions decrease risk of aspirations Diagnosis: SCHIZOPHRENIA Treatment: Antipsychotic/Neuroleptics Side Effects: Tardive Dyskinesia, Pseudoparkinsonism, Neuroleptic Malignant Syndrome (NMS), Akathisia, Dystonia, and Anticholinergic Side Effects: Constipation, Retention of Urine, Dryness of Mouth, Decrease Urine Output  SYMPATHETIC NERVOUS SYSTEM | ADRENERGIC Alpha 1 Alpha 2 Beta 1 Beta 2 Blood Vessels CNS Nerve Membrane Heart Lungs Vasoconstriction Decrease NE release Increase HR Bronchodilation Urinary Bladder Weakens SNS Increase Contractility Uterus Retention of Urine PSNS Response Kidney Relaxation Iris Pancreas Increase Renin release Blood Vessels Dilation: Mydriasis Decrease Insulin release Vasodilation Hyperglycemia Liver Glycogenolysis Hyperglycemia Alpha-1 Adrenergic Alpha-2 Adrenergic Beta-2 Adrenergic Agonist Agonist Agonist Phenylephrine Clonidine (Catapres) Albuterol/ Salbutamol SNS response Crosses BBB BP (Ventolin) No effect on HR Used in Used in hypertension SNS Effect bronchoconstriction Used in an eye exam Vasoconstriction (asthma) Used in hyperkalemia ACTIONS: HR TPR BP A.K.A. Short Acting Decongestant Beta Agonist (SABA) Blood Vessels Methyldopa Used for emergency Used in Hypertension rescue inhaler Vasoconstriction Side Effect: Side Effects: palpitation Hypotension & tremors Blood Flow Cells Shrink Terbutaline (Bricanyl) Vasopressor Used in asthma & Vasoconstriction COPD Tocolytic: blocks TPR BP muscle contraction: used in premature Alpha Adrenergic Agonist labor: uterine muscle Midodrine Formoterol (Salmeterol) Used in chronic orthostatic LABA hypotension Used in preventing SNS Effect: Vasoconstriction – Inc HR, future attacks of TPR, and BP asthma. Alpha 1 Adrenergic Alpha Adrenergic Antagonist Antagonist Beta-Adrenergic Blockers Prazosin Phentolamine Propranolol Used in Hypertension Pharmacodynamics: for tachycardia in hyperthyroidism Vasodilation TPR BP Vasodilation TPR BP for stage fright Used in Hypertensive Crisis prophylaxis in migraine Doxazosin due to: Timolol Used in Hypertension Pheochromocytoma For Open-Angle Glaucoma, by decreasing the Emptying of the (Tumor in Adrenal Medulla) production of aqueous fluid dec IOP bladder for BPH Secretes NE SNS BP Prophylaxis for migraine (eye drops) MAOIs Increase NE BP Nadolol DOC for Angina + Hypertension Terazosin Used in Hypertension Side Effects Contraindications/ NC Emptying of the Bradycardia Hold if HR < 60bpm bladder for BPH Hypotension Hold if BP 20mmol/L (Initial side effects: nausea) >30mmol/L (late sign: tremors) e.g. Caffeine Aminophylline Theophylline FOR INFLAMMATION GLUCOCORTICOIDS LEUKOTRIENE MODIFIERS CROMOLYN SODIUM Effects: Anti-Inflammatory Promotes smooth muscle constriction Inhaled Medication Immunosuppressant and inflammatory response Stabilized mast cell (histamine-containing cell) Normally produced by the Added on when glucocorticoids aren’t Suppresses inflammation adrenal cortex in the body. enough Not relieve Can be given as medication bronchoconstriction by Inhaled, Oral, IV e.g. Montelukast “Preventers” Uses: Prevent asthma attack Given on fixed schedule, not PRN Suppress inflammation (not for emergency) Less mediators released (leukotrienes, histamine, PG) Less edema in airway mucosa Fever inflammatory responders (eosinophils, leukocytes)  GASTROINTESTINAL DRUGS Mucus – coat the lining Bicarbonate – neutralizes gastric acid Prostaglandin – stimulates mucus and bicarbonate secretion CAUSES: H. pylori – most common NSAIDs – inhibit prostaglandin (Mefenamic, Alaxan, Skelan) PEPTIC ULCER DISEASE Gastric Acid (HCl) injures the mucosa cells and activates pepsin Smoking and Alcohol gastric acid, bicarbonate production delays healing DRUGS AFFECTING GASTRIC SECRETIONS Drugs for PUD, Gerd, And Gastritis PROTON-PUMP HISTAMINE-2 GASTROINTESTINAL PROSTAGLANDIN ANTACIDS INHIBITOR (PPI) RECEPTOR BLOCKER PROTECTIVES Aluminum Hydroxide Releases HCl Produce HCl Coats Ulcer Agonist SE: Constipation NC: Take before Omeprazole Cimetidine meals Misoprostol Magnesium Hydroxide Pantoprazole Ranitidine (Cytotec) SE: Diarrhea Ozemeprazole Famotidine Sulfacrate