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RespiratoryDrug ClassesDrugsMechanism of ActionAnti-Tuberculosis DrugsTuberculocidalIsoniazid CYP450 Inhibitor Metabolize through acetylation, highly genetic polymorphism Side Effects Peripheral neuropathy – supply Vit B6Hepatotoxic Mycolic Acid synthesis inhibitor Spectrum of Activities Kill extracellular bacteria Weakens intracellular bacteria Rifampicin CYP450 Inducer in HAART, change with Rifabutin Side Effects Orange discoloration of body fluid Bind to B subunit of RNA polymerase, inhibit mRNA synthesisSpectrum of Activities Kill Extracellular bacteria Intacellular organism Spurters Pyrazinamide Side Effects Hyperuriceamia Fatty Acid Synthase inhibitor Spectrum of Activites Weakly kill intracellular bacteria Streptomycin Side Effects Ototoxic Nephrotoxic Bind to 30S ribosomal subunit, inhibit protein synthesisSpectrum of Activities Kill only extracellular bacteria TuberculostaticEthambutolSide Effects Optic NeurittisContraindicated in very young children Arabinogalactan synthesis inhibitor Drugs for COPDBronchodilatorsBeta2 AgonistsSalbutamol – rapid onset, short duration Salmeterol – slow onset, long duration Binds to Beta 2 receptors, stimulate Adenylate Cyclase Methylxantine – Theophylline Narrow Therapeutic Index Toxic Effects Fatal arrhythmias Fatal convulsion Phosphodiesterase III inhibitor Antimuscarinic Agent – Ipratropium BromideCompetitively blocked M3 receptor of bronchiol smooth muscle cells, inhibit Phospholipase CAntiinflammatoryAgentsCorticosteroid 1.Prednisolone – oral 2.Hydrocortisone – IV 3.Beclamethasone – inhalationInhibits Phospholipase A2 in which involve in the formation of Arachidonic AcidMast Cells Stabilizer – Cromone Inhibits the release of inflammatory mediators from mast cellsLeukotriene Receptor Antagonis Montelukast Zafirlukast Selectively block Cysteine Leukotriene (LT) receptorLeukotriene Synthesis Inhibitor – ZileutonInhibits lypoxygenase enzyme which involves in the coversion of Arachidonic acid to LeukotrieneMucolyticsN-acetylcysteine/ Ambroxol Splitting the disulfide bond that links proteins in the mucusMusculoskeletalDrug ClassesDrugsMechanism of ActionNSAIDsNon-Selective COX InhibitorAspirin Displace Warfarin from AlbuminContraindication Relative C/IAsthma Absolute C/I Gouty ArthritisChildren – Reye Syndrome Pregnant Irreversibly and non-selectively both COX1 and COX 2Selective COX2 InhibitorCelecoxib Side Effects Cardiovascular side effects Selective COX2 inhibitor Anti-GoutSymptomatic RelieveCorticostreroid Side Effects Osteoporosis Cushing syndrome Inhibits Phospholipase A2 in which involve in the formation of Arachidonic AcidCOX2 selective NSAIDsDiclofenac sodium Celecoxib Indomethecin Selective COX2 inhibitorColchicine Low Therapeutic Index Side Effects Intractable diarrhea ↓leukocytes migration and release of inflammatory mediators by binding with intracellular tubulin, inhibiting its polymerizationAnti-Hyperuriceamic AgentsAllopurinol – overproducer Interaction with Azathioprine (requires Xanthine Oxidase for metabolism)Xanthine Oxidase inhibitor Uricosuric Agents – undersecretor Probenecid SulfinpyrazoneUricosuric drugs act by affecting the active transports so that the net reabsorption of uric acid will be ↓DMARDsMethotrexate Side Effects 1.Mucosal toxicity 2.Myelosuppression 3.HepatotoxicityIrreversible inhibition of Dihydrofolate reductase (DHFR) Partially reversible inihibiton of Thymidylate synthetase Inhibition of Aminoimidazolecarboxamide Ribonucleotide Transformylase (AICAR) Sulfasalazine Side Effects Steven Johnson syndrome Suppression of T cell and subsequently leading to ↓in B cellsInhibits the release of inflammatory cytokines which are produced by macrophages and monocytesHydroxychloroquine Contraindicated in G6PD deficiency Uncertain Leflunomide CYP450 Inhibitor TERATOGENIC inhibit Dihydroorotate Dehydrogenase, an enzyme requires for synthesis of ribonucleotideBiological Agents (Not DMARDs)TNF-a Antibodies Humanized – Adalimumab Chimeric – Infliximab Form complex with soluble TNF-a, therefore prevents its interaction with p55 and p75 receptors on various tissuesSoluble TNF-a Receptors – Etanercept Binds with TNF-a therefore inhibiting it from binding to bound receptorIL-1 Receptor Antagonist – AnakinraCompetitively inhibiting the binding of IL-1 to the Interleukin-1 type receptorCardiovascularDrug ClassesDrugsMechanism of ActionChronic Isheamic Heart Disease Therapeutic InterventionNegative Inotropic, Chronotropic and Dromotropic AgentsNon-Selective Beta Blocker – Propanolol Contraindication Asthma COPD Heart block Peripheral heart disease Blocks both Beta 1 and Beta 2 receptors If Channel Blocker – Ivabradine Block the HCN channel/ Funny channelCalcium Channel Blocker Benzothiazepine Diltiazem – arteriole and heart Phenylalkylamine Verapamil – heart only Contraindication Sinus bradycardia AV conduction defect Severe cardiac failure Blocks the Ca channel Inhibit the release of Ca and leads to inhibition of interaction between Myosin and actinInhibits muscle contraction Agents Reducing AfterloadCalcium Channel Blocker Dihydropyridine Nifedipine – arterioles only Agents Reducing Afterload and PreloadNitrates Glycyltrinitrate – sublingual For acute attack Isosorbide-5-mononitrate – oral For prophylaxis Contraindication ICP Hypotension Severe hemolytic anemia Drug interaction Viagra – severe hypotension Release Nitric Oxide, activating GuanylylcylaseDevelops tolerance quickly Nicotinamide Nitrate Ester – Nicorandil Activate potassium channel Anti-Ischeamic Metabolic AgentTrimetazidine ↑myocardial glucose utilization through inhibition of fatty acid metabolismAntiplateletAspirin Nonselective COX inhibitor CardiovascularDrug ClassesDrugsMechanism of ActionAcute Coronary Syndrome Therapeutic InterventionImmediate TreatmentFibrinolytics and ThrombolyticStreptokinase – non-fibrin specific Streptokinase is given in order to bind to the Plasminogen, which in return will allow Urokinase to cleave Plasminogen into Plasmin. Then, protect the Plasmin from being deactivated by plasma Anti-PlasminAlteplase – Fibrin specific Stimulates Plasminogen leading to clot dissolution ProphylaxisAntiplateletAspirin Nonselective COX inhibitor ADP Receptor Antagonist Ticlopidine – cause Neutropenia Clopidogrel – not cause Neutropenia non-competitive ADP receptor inhibitorInhibits platelete aggregation ↓platelets conformational change ↓release of platelet granules↓platelet amplification Dipyridamole 1.Inhibits Thromboxane Synthase 2.Inhibits the reuptake of Adenosine 3.Inhibits PhosphodiaesteraseGlycoprotein IIb/IIIa Platelet Membrane Receptor BlockerAbciximab Block receptor, stopping the common ligands from activating the complex. This will therefore lead to a.Blocks formation of fibrin b.Inhibits platelet aggregationAnti – Hyperlipideamic AgentsHMG-CoA Reductase Inhibitor – Simvastatin Side Effects Rhabdomyolisis Hepatotoxic Inhibits HMG-CoA Reductase enzyme, use in conversion of ACoA to Mevalonic Acid ACoA Mevalonic Acid TG Vitamin B3 (Niacin) – Nicotinic Acid Side Effects Hyperglyceamia Magnifies the activity of Lipoprotein Lipase of adipose tissuesFibrates – Gemfibrozil Displace Warfarin from Albumin Side Effects Rhabdomyolitis – if given with Statins Gallstone Hepatotoxic Fibrate is a ligand of nuclear transcription factor; PPAR-aStimulates Lipoprotein Lipase Bile Acid Sequestrants – Cholestyramine Binds to bile acid in the gut, reduces bile acid reabsorption as high as ten foldsIntestinal Sterol Absorption Inhibitor – Ezetimibe Selective inhibitor of transport protein NPCL1L1, important in the absorption of a.Cholesterol b.PhytosterolsCardiovascularDrug ClassesDrugsMechanism of ActionAntiarrhythmic AgentsClass 1Sodium Channel BlockersClass 1aQunidine Procainamide Side Effects Cinchonism Contraindication – Acute heary failure Displace Warfarin and Digoxin from Albumin 1.Blocks Na+ channels 2.Blocks K+ channels 3.Blocks Alpha receptorsUsage 1.Supraventricular arrhythmias 2.Ventricular arrhythmiasClass 1b Lidocaine 1.Low effect on blocking Na+ channel 2.↑K+ conduction 3.No effect on cardiac contractilityUsage Ventricular arrhythmias only Class 1c Flecainide Propafenone The most potent Na+ channels blocker Does not have any activity on K+channel Some degree of beta receptors blockageUsage 1.Supraventricular arrhythmias 2.Ventricular arrhythmiasClass 2Beta BlockersBeta Adrenergic Blocking Agent Propanolol Esmolol Metaprolol Blocking the Beta receptor especially Beta 1 receptors on the heart will inhibit the stimulation of sympathetic of the heartUsage 1.Supraventricular arrhythmias 2.Ventricular arrhythmiasClass 3Potassium Channel BlockersIbutilide Pure Potassium channel blocker Amiodarone CYP450 Inhibitor Highly risk to get Torsades de Pointes Side Effects 1.Pulmonary fibrosis 2.Impaired thyroid function 3.Blue-grey discoloration of skin4. Impaired liver function 5.Corneal micro-deposit1.Blocks Na+ channels 2.Blocks Beta adrenegic receptors 3.Blocks K+ channels 4.Blocks Ca2+ channelsUsage 1.Supraventricular arrhythmias 2.Ventricular arrhythmiasClass 4Calcium Channel BlockerCalcium Channel Blocker Verapamil – heart Diltiazem – arteriole and heart Blocks L type Ca2+ channelsUsage Supraventricular arrhythmias only Haemopoetic and LymphaticDrug ClassesDrugsMechanism of ActionImmunopharmacologyCorticosteroidInhibits Glucocorticoid Response Element (GRE) of DNA. Interleukin Synthesis InhibitorCalcineurin InhibitorCyclopsporineCYP450 Inhibitor and Inducer Binds to Immunophylin, the complex is then makes Calcineurin to be dysfunctional Tacrolimus Binds to FKBP-12, the complex then makes the Calcineurin to be dysfunctional mTOR (Mammalian Target of Rapamycin) InhibitorSirolimus/ Rapamune Sirolimus will binds to Immunophilin and this Sirolimus-Immunophilin complex will inhibit the mTOR actvitiyImmunosuppressive Antiproliferative/Antimetabolite AgentsMycophenolate Mofetil Inhibits the Inosine Monophosphate (IMP) Dehydrogenase enzymeImmunosuppressive AntibodiesMurine (Rat) Monoclonal AntibodyMuromonab-CD3 (OKT3)Muromonab will bind to CD3 protein on the T cells, inhibiting lymphocyte function as access to antigen recogition site isThymoglobulin Antithymocyte Globulin RabbitAntibody binds to surface of the circulating T cellsIL-2 Receptor Antibodies Daclizumab – HumanizedBasiliximab – Chimeric Binds to IL-2 receptor alpha subunit on activated T cellAnticancer DrugsAlkylating AgentsCyclophospamide Binds covalently with DNA, leading to DNA fragmentation Cross bridges formation Mispairing of Nucleotides AntimetabolitesFolate Antagonist – Methotrexate Irreversible inhibition of Dihydrofolate reductase (DHFR) Partially reversible inihibiton of Thymidylate synthetase Inhibition of Aminoimidazolecarboxamide RibonucleotidePyrimidine Analogue – 5-Flurouracil Inhibits Thymidylate Synthase Inhibits RNA Polymerase Purine Analogues Azathioprine – prodrug 6-mercaptopurine – active metabolite Inhibits enzymes involved in purine synthesis Plant DerivativesVinca Alkaloid Vincristine – from Vinca rosea Paclitaxel – from European yewBinds to tubulin and inhibits its polymerization into microtubuleAntitumour AntibioticsDoxorubicin Side Effects Cardiotoxicity Interact with DNA by intercalation and inhibition of macromolecular biosynthesis.Haemopoetic and LymphaticDrug ClassesDrugsMechanism of ActionAntimalarial DrugsClass 1Asexual Erythrocytic stageChloroquine Contraindicated in G6PD deficiency Long half life, use loading dose Resistance develops in P.falciparum Inhibit the biocrytallization of heme into hemozoine leading to build up of heme in the vacuole which toxic to parasite Spectrum of Activities Highly effective blood schizonticide Moderately effective against gametocytes P. vivaxP.malariae P.ovale NOT P.falciparum CANNOT against hepatic stage parasite Quinine Contraindicated in G6PD deficiencyLong half life, use loading dose Side Effects Quinine triads Cinchonism Hypoglyceamia Hypotension Unknown Spectrum of Activities Highly active blood schizontycide Gametocidal to P.vivaxP.ovalae NOT P.falciparumArtemisnin Compound Artesunate – water soluble Artemether – lipid soluble Dihydroartermisnin – water soluble Production of free radical in the food vacoules Inhibition of Ca2+ATPase pump of the parasiteSpectrum of ActivitiesRapidly acting blood schizonticide Folate Antagonist Combination Fansidar Pyrimethamine Pyridoxine Side Effects Steven Johnson syndrome Contraindication Pregnancy and baby – Kernicterus Sulfadoxine inhibits Dihyropteroate Synthase enzyme Pyrimethamine inhibits the Dihydrofolate Reductase enzyme Spectrum of Activities Slow acting blood schizonticide Tetracycline Contraindication in pregnancy and baby due to permanent teeth discoloration Binds to 30S ribosomal subunit Blocks tRNA binding to A site Spectrum of Activities Slow acting blood schizonticides Class 2Primary Hepatic and Eryhtrocytic StageAtavaquone Acts by interfering with the parasitic mitochondrial functionClass 3Primary and Secondary Hepatic StagePrimaquine Contraindicated in G6PD deficiency Unknown Spectrum of Activities The only antimalarial can fight againt hepatic latent and primary stage No activity against erythrocytic stageCentral Nervous SystemDrug ClassesDrugsMechanism of ActionOpioid Analgesic and AntagonistStrong Opioid AgonistMorphine Strong ? (Mu) agonist Variable affinity towards ? (Delta) receptor k (Kappa) receptorFentanyl Methadoneless severe withdrawal syndrome use in management of dependency Meperidine Used in Biliary colic Strong k (Kappa) receptor agonist Antimuscarinic Distinctive anticholinergic effectPartial Opioid AgonistCodeine Partial agonist of ? (Mu) receptorDextrometorphan Suppress cough center at Medulla Oblongata Partial ? (Mu) receptor Antagonist the activity of NMDA glutaminergic receptor Inhibit reuptake of serotoninMixed Receptor AgonistsPentazocine k (Kappa) receptor agonist Antagonist in ? (Mu) receptor ? (Delta) receptorOpioid AntagonistsNaloxone Used in Opioid toxicity NOT dependency Inhibits all opioid receptors ? (Mu) receptor ? (Delta) receptork (Kappa) receptorOther Non-Opioid AnalgesicTramadol Weak ? (Mu) receptor agonistModerate Serotonin Reuptake Transporter (SERT) inhibitor Weak Norepinephrine Reuptake Transporter (NET) inihibitorCentral Nervous SystemDrug ClassesDrugsMechanism of ActionAntiepileptic DrugsPhenytoin CYP450 Inducer Contraindicated in pregnancy – Fetal Hydantoin syndrome Narrow Therapeutic Index Follow zero order elimination Displace drugs from Albumin Side Effects Nystagmus Ataxia Diplopia Gingvial hyperplasia Blocks the activated state of Na+ voltage channels ↓synaptic release of GlutamateIndication Generalized tonic-clonic/ Gran mal seizure Partial seizures Should not be given in Absence seizures Carbamazepine CYP450 Inducer Contraindicated in pregnancy Valproic Acid CYP450 Inhibitor Displace Phenytoin from Albumin Contraindicated in pregnancy Blocks the activated state of Na+ voltage channels Blocks the NMDA receptors ↑GABA level in the brain Indication Generalized tonic-clonic/ Gran mal seizure Partial seizures Generalized seizures Absence seizures Myoclonic seizures Felbamate Block of NMDA receptors ↑GABAA receptor responsesIndicationsPartial seizures Generalized seizuresEthosuximide ↓the low-threshold current of Ca2+ T-type channelsIndication Absence seizure Phenobarbital ↑phasic GABAA phasic receptor responses ↓excitatory synaptic responses Indications Generalized tonic-clonic/ Gran mal seizure Partial seizures Generalized seizures Neonatal seizures Status epilepticusBezodiazepine Diazepam Clonazepam ↑phasic GABAA phasic receptor responsesIndication Diazepam Status epilepticusClonazepam Absence seizures Myoclonic seizure Infantile spasmTopiramate Blocks the activated state of Na+ voltage channels Indications Generalized tonic-clonic/ Gran mal seizure Partial seizures Generalized seizures Absence seizuresLamotrigine Prolong inactivation of Na+ voltage channels Blocks presynaptic Ca2+ voltage channels ↓release of GlutamateIndicationsGeneralized tonic-clonic/ Gran mal seizure Partial seizures Generalized seizures Absence seizures Myoclonic seizuresCentral Nervous SystemDrug ClassesDrugsMechanism of ActionGeneral AnasthesiaBarbiturate – Thiopental Contraindicated inSevere hypotension Addison disease Liver disease Breathing disorder Lipid Solubility-Anaesthetic Potency Correlation (the Meyer-Overton correlation)Lipid Hypotheses of General Anaesthetic ActionModern Lipid HypothesesMembrane Protein Hypothesis of General Anaesthetic actionBenzodiazepine Contraindicated in PregnancyMyasthenia gravis COPDPropofol Etomidate Ketamine Contraindicated in ICP Local AnasthesiaAmideMedium action Lidocaine Long action Bupivacaine Inactivation of Sodium channel trhough closure of M type channel and eliciting Potassium influx EsterShort acting Procaine Long action Tetracaine Surface acting Cocaine Anti-ParkinsonismLevodopa Given with carbidopa to inhibit the action of peripheral DOPA Decarboxylase L-Dopa is the precursor of Dopamine; therefore by administering L-Dopa with hope it will increase the level of Dopamine in the brainMAOb Inhibitor Selegiline Covalently bind to MAOB and leads to irreversible inhibition of the activity of the enzymeCOMT Inhibitor Tolcapone – not used anymore due to severe Hepatotoxicity Entacapone COMT inhibitors are somehow similar to that of Carbidopa, in a sense that COMT inhibitors inhibit the activity of COMT in the periphery as well as in the brainDopamine Receptor AntagonistBromocriptine Other Usage Hyperprolactineamia GalactorrheaAmenorrhea Type 2 Diabetes Mellitus Potent agonist at dopamine D2 receptors and various serotonin receptorsAnticholinergic Agent Benzatropine Antagonises the effect of acetylcholine, decreasing the imbalance between the neurotransmitters acetylcholine and dopamineCentral Nervous SystemDrug ClassesDrugsMechanism of ActionSedatives and HypnoticsHypnotics Barbiturate – PhenobarbitalCYP450 Inducer Side Effects Hangover syndrome DependenceWithdrawal syndrome Tolerance Increase the mean open time of GABA-A activated chloride channelsBenzodiazepine – Clonazepam Flumazenil used in Benzodiazepine toxicity Binds to Alpha1 and Alpha2 Benzodiazepine sites on the GABA receptorsNewer HypnoticsZolpidem Selectively binds to the Alpha1 site on the GABA receptorsAnxiolyticsBuspirone Partial agonist of the 5-HTA1 Serotonin receptors Has also affinity towards D2 Dopaminergic receptorsAntipsychotic and LithiumTypical AntipsychoticHaloperidolSide Effects Extrapyramidal side effects Acute dystonia Akathasia Parkinsonism Tardive dyskinesia Nacoleptic Malignant Syndrome Competitively inhibits the D2 receptorsAtypical AntipsychoticClozapine Side Effects Agranulocytosis Cardiac toxicity DKA Preferentially inhibit D4 receptor Partial agonist of 5-HT1A and 5-HT1B Mood StabilizerLithium Narrow Therapeutic Index Side Effects Diabetes Insipidus Thyroid toxicity Attenuate the signalling via Phosphotidyl Biphosphate (PIP2) 2nd messenger coupled receptorsAntidepressantTricylic Antidepressant Primary Amine – Amitriptylline Secondary Amine – Desipramine Inhibition of Norepinephrine and Serotonin reuptakeInhibit presynaptic transporters Serotonin Transporter (SERT)Norepinephrine Transporter (NET)MAO Inhibitor – Phenelzine Serotonin syndrome if given with SSRI Cheeze effect when taken with tyramine containing foods Nonselective MAO A and MAO B inhibitor Selective Serotonin Reuptake Inhibitor – Fluoxetine SELECTIVELY inhibits the action of Serotonin Transporter (SERT)Serotonin/Norepinephrine Reuptake Inhibitor – Venlafaxine Potent inhibitor of SERT and NET Atypical Antidepressant – Bupropion Inhibits the reuptake of Norepinephrine and Dopamine Stimulates the release of Dopamine and Norepinephrine from the presynaptic terminal Urinary Drug ClassesDrugsMechanism of ActionTreatment of UTIFluoroquinolone (Bacteriocidal)Contraindicated in Pregnancy Children below 18 years old Side Effects Photodermatitis Abnormal bone and cartilage growth Tendonitis CNS toxicity CVS toxicity QuinoloneNalidixic Acid Gram Negative except P.aeruginosa No Gram Positive Inhibits DNA Gyrase and Topoisomerase IV FlouroquinoloneCiprofloxacin (2nd Generation)Gram Negative Gram Positive except Strep. Pneumoneae Levofloxacin (2rd Generation)Gram Negative Gram Positive Atypical bacteria Moxifloxacin (4th Generation)Gram Negative Gram Positive Atypical Bacteria UrosepticNitrofurantoin (Bacteriocidal)Contraindicated in pregnancy and G6PDThis electrophilic intermediate will non-specifically attack Bacterial ribosomal protein DNA Respiration Pyruvate metabolism Other macromolecules Inhibition of protein synthesisFosphomycin (Bacteriocidal)The first stage of cell wall synthesis takes place in the bacterial cytoplasmAminoglycosides, Sulfonamides and TrimethoprimAminoglycosides Streptomycin, Gentamicin Post antibiotic effect, use loading dose It binds to the 30S Ribosomal Subunit of bacteria, thus inhibiting protein synthesis Trimethoprim and Sulfamethoxazole (Bactrim)Contraindicated in pregnancy and infant – Kernicterus G6PD Ratio 1:5, trimethoprim and sulfonamide Sulfonamide inhbits Dyhropteroate Synthase Trimethroprim inhibits Dihydrofolate Reductase ................
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