Directly Acting Cholinomimetics / Acetylcholine / Degraded by Ach-esterase and recycled / Stimulates muscarinic and nicotinic receptors / None – stimulates all autonomic ganglia / General Muscarinic:
Salivation,
↑bronchial + GI secretions, blurred vision,
sweating,
hypotension,
bradycardia.
Bethanecol / t½=3-4hrs
limited access to brain / Muscarinic agonist, especially M3(glands) / ↑Bladder emptying + GI motility
Pilocarpine / t½=3-4hrs
not Ach-esterase substrate / Muscarinic partial agonist / Glaucoma (local admin) / Pupil constriction aids fluid drainage
Indirectly acting Cholinomimetics
Anticholinesterase / Physostigmine / t½=30mins
ANS>NMJ / Reversible AChE inhibitor. Block active site with carbamyl group.
Reactivated by hydrolysis / Glaucoma (local), Atropine poisoning / Low: ↑Muscarinic effects
Moderate: ↑ANS / General Muscarinic
Higher doses - ↑all ANS, depolarising block
Neostigmine / Myasthenia gravis
Ecothiopate (organo-phosphorous compounds) / Irreversible AChE inhibitor. Phosphorylates enzyme (stable) / Glaucoma (local)
[Insecticides] / SLUDGE BBB / Excitation, convulsions, unconsciousness, resp depression, death.
Antidote: PralidoxinBBB
Cholinoceptor Antagonists / Trimetaphan / IV / Nicotinic ion channel blockers (incomplete, use dependent)
[Ganglion Blocking] / To induce hypotension during surgery / Hypotension, vasodilation, ↓Renin secretion. / ↓↓ANS function. Death due to targeting skeletal muscle.
↓Secretions, pupil dilation, ↓GI tone, bronchodilation
Hexamethonium / Anti-hypertensive
(not in use)
Atropine / I.V. after MI / Muscarinic antagonist / Parkinson’s disease, IBS, MI (↓motility+secretions) / Cholinergic balance in basal ganglia / Mild doses – agitation, ↓sweating, ↓secretions, Cylopegia, CNS disturbance, drowsiness, mydriasis, constipation at high doses
Poisoning: Hyperactivity -> CNS depression.
Hot, Dry, Blind, Mad:
Treat with anticholinesterase
Hyoscine
(Anti-emetic) / Transdermal patch, oral, I.V. / Muscarinic antagonist. Acts at vestibular nucleus, NST, vomiting centre. / Anaesthetic premedication, prevents motion sickness (not during) / Sedation at mild doses, bronchodilation
Tropicamide / Local / Muscarinic antagonist / Examination of retina / Pupil dilation
Ipratropium bromide / Inhalation / Muscarinic antagonist / Asthma, obstructive airway disease / Bronchodilation
Neuromuscular blocking drugs
(non-depolarising) / Tubocurarine / I.V. (↑ charged) doesn’t cross BBB/ placenta. Not metabolised. Excreted 70% urine, 30% bile. / Competitive AChR antagonist at NMJ.
70-80% block necessary.
Graded block – greater block further away from endplate. / Relaxation of skeletal muscle during surgery. ↓need for anaesthetic and permits artificial ventilation. / Flaccid paralysis – eye muscles, face, limbs, diaphragm / Hypotension (↓TPR, histamine release), reflex tachycardia, bronchospasm, excessive secretions, apnoea – must assist respiration. Can be reversed by anti AChE
(non-depolarising) / Atracurium / Duration – 15-60m
Spon Decompose / See above / See above / Histamine: Bronchospasm, Excessive Secretion + HypoT
Depolarising Neuromuscular Blockers / Suxamethonium / Not broken down by AChE. Hydrolysed by Pseudo-cholinesterases. DOA – 3-7mins / AChR agonist. 2 ACh molecules.
Steady influx of Na+ means inactivation remains closed, as potential cannot fall below threshold. / Brief procedures – tracheal intubation, dislocations. / Flaccid paralysis / Muscle pain, loss of K+, bradycardia
SNS Agonists
(sympatho-mimetics)
Direct / Adrenaline / I.V., I.M., local
Poor oral absorption.
DOA – mins – quickly degraded / Non-selective (αβ) / Anaphylactic shock, COPD, heart block management, spinal anaesthesia, prolong DOA of local anaesthesia, glaucoma / Bronchodilation, suppression of mediators, ↑HR + contractility, ↑TPR, vasoconstriction / Secretions: ↓mucus, thicker
CVS: cold extremities tachycardia, palpitations, arrhythmias, stroke pulmonary oedema
Muscle: Tremor
Phenylephrine / Resistant to COMT, not MAO.
Usually local admin / Selective α1 agonist / Vasoconstrictor, mydriatic, nasal decongestant / Pupil dilation, restricts blood to prevent mucus production / CVS effects
Clonidine / Oral, I.V. / Selective α2 agonist
↓Sympathetic tone by pre-synaptic NA inhibition / Hypertension, migraine / ↓Sympathetic outflow from brainstem
Isoprenaline / Resistant to Uptake 1 and MAO. t½=2hrs I.V. / Selective β1+β2 agonist / Heart block, cardiogeneic shock, acute heart failure, MI (No longer for asthma) / Reflex tachycardia, dysrhythmias
Dobutamine / t½=2min, rapid COMT degradation. I.V. / Selective β1 agonist / Heart block, cardiogeneic shock, acute heart failure, MI / No reflex tachycardia
Salbutamol / Resistant to COMT, MAO, Uptake 1. I.V., oral, inhalation / Selective β2 agonist / Asthma
Threatened uncomplicated premature labour / Bronchodilation, inhibition of mediators / Reflex tachycardia, tremor.
Caution in cardiac patients, hyperthyroidism and diabetics
SNS Agonists
(sympatho-mimetics)
Indirect / Tyramine / In cheese, wine, soy sauce.
Extensive 1st pass metabolism, short half life. No BBB / Weak non-selective agonist
Competitive Uptake1 inhibitor
MAO Competitor. Displaces NA from vesicles into cytosol causing NA leak from cell. / - / - / Hypertensive crisis “Cheese Reaction” when taking MOA inhibiting drugs
Indirect sympatho-mimetic,
Drug of abuse,
Local Anaesthetic / Cocaine / Smoked – absorbed quickly, slow orally, nasally. Well absorbed. Readily crosses BBB. Degraded by plasma + hepatic esterases. 90% protein bound t½=30mins. Excreted in urine. / Uptake 1 inhibitor.
Prevents NA reuptake therefore ↑ Synaptic Activity
Prevents re-uptake of Dopamine in NAcc.
Blocks voltage gated Na+ channels. / Local anaesthetic in ophthalmology.
Do not co-administer with Adrenaline / Euphoria, excitement, ↑motor activity, tachycardia, vasoconstriction, ↑BP, HR, platelet activation, tremors, convulsions, resp depression (medullary centres), death
SNS Antagonists / Propranolol / β1+β2 antagonist / Anxiety
Hypertension, Arrhythmias, Angina, Glaucoma / ↓CO, + BP during exercise / Bronchoconstriction,
Cardiac Failure, Hypoglycaemia
Fatigue, Cold Extremities, Bad Dreams
Atenolol / Not for Asthmatics / β1 antagonist / ↓CO, effect on airways only in high doses
Labetolol / β1+α1 antagonist / ↓TPR, no change in CO
Phentolamine / α1+α2 antagonist / Not used / ↓BP, TPR, reflex ↑CO/HR / ↑NA release due to α2 blockade, reflex tachycardia, ↑GI motility, diarrhoea
Prazosin Doxazosin / α1 antagonist / Hypertension / ↓BP/, ↓CO, VD dramatic hypotension, ↓LDL and ↑HDL / Postural hypotension
False Transmitters / Methyldopa / Not degraded by MAO. Doesn’t cross placenta / Taken up by NA neurones, forms false transmitter. Less active on α1, more active on α2. Accumulates in neurone. / Hypertension
(in pregnancy) / Renal blood flow well maintained – good in renal failure. / Dry mouth, postural hypotension, sexual dysfunction, sedation
Hepatitis-like damage.
Drugs affecting rennin – angiotensin – aldosterone system / Enalapril, Captopril / Inhibit ACE, prevent conversion of angiotensin I to angiotensin II / Hypertension, heart failure, post-MI, diabetic nephropathy, renal insufficiency. / Prevent vasoconstriction→↓TPR→↓BP / Hypotension, dry cough, angioedema, hyperkalaemia, renal failure
Losartan / Non-competitive antagonist of Angiotensin 1 receptors. / Hypertension. Patients with heart failure that cannot tolerate ACEIs / Less extensive than ACE inhibitors
Aliskiren / Inhibits Enzyme (Renin) / Experimental
Calcium channel Antagonists / Verapamil / Phenylakylamine / Inhibit opening of L-type calcium channels. Causes arterial vasodilatation / Angina, Hypertension, SVT, atrial fibrillation / ↓HR (AV) and contractility. / AV block, bradycardia, heart failure, constipation
Diltiazem / Benzothiazepine / Angina, Hypertension / ↓cardiac workload / Flushing, headaches, hypotension, ankle oedema
Amlodipine / Dihydropyridines / Hypertension
Βeta-Blocker / Atenolol / No longer 1st line
Hypertensive / β1 Antagonist / Angina, Cardiac dysrhthmias, HF, Thyrotoxicosis, Glaucoma, Mirgane / -ve Chronotropic & inotropic
Control/Correct Dysrhythmia / Bronchoconstriction, heart block, bradycardia, fatigue, cold extremities, nightmares, hypoglycaemia in diabetics
Organic Nitrates / Glyceryl Trinitrate / Extensive 1st pass metabolism. t½=30mins, sublingual, oral.
Latter 2 longer transdermally. / Release NO→venodilation ↓venous return. Weak antiplatelet, coronary artery VD / Angina / Improve myocardial oxygen demand / Hypotension, headache, flushing,
Tolerance – Eccentric dosing.
Nicorandil
Isosorbide Mononitrate / Opens K+ channels→ arterial dilation. Also NO donor.
Anti-arrhythmics / Adenosine / t½=20-30s
I.V. / Acts on A1 receptors to slow conduction through AV node / Terminate SVT, safer than verapamil / Chest pain, SoB, dizziness, nausea.
Amiodarone
Dronedarone / t½=10-100days
D: Less toxic but less effective / Complex ion channel blocker / SVTs and ventricular tachyarrhythmias. / Accumulates in skin, lungs, thyroid. Photosensitive skin rash, pulmonary fibrosis.
Digoxin
(Cardiac Glycosides) / t½=40hrs / Inhibit Na+/K+ pump. ↑intracellular Na+→↑Ca2+ via Na+/Ca Exchange →
+ve inotropic effect.
Central Vagal Stimulation ->
-ve chronotropic / Atrial fibrillation, relief of symptoms in heart failure. / ↓Ventricular rate, ↑contractility. Slows conduction through AVn / Amiodarone and verapamil ↓digoxin excretion and tissue binding. Immune antibody available for toxicity.
AV block and ectopic pacemaker.
Ivabradine / CI: post-MI, sick sinus syndrome; cardiogenic shock; / Blocks If channel – Na/K channel in sinoatrial node / Angina (w/ normal sinus rhythm) / Slows HR / Bradycardia, 1 degree Heart block, Ventricular & SVA
Cardiac Intropes / Dobutamine / β1 selective agonist / Positive Inotroic:
↑ Force of Contractions
Milrinone / Phosphodiesterase Inhibitor: Prevents cGMP breakdown / Decrease chronic heart failure survival rate
α-blockers + sympatholytics / Doxazosin
Prazosin / Competitive α1 antagonist / Postural Hypotension
Phenoxybenzamine / Irreversibleα1 antagonist / Pheochromocytoma (w/ β-blockers) / Tachycardia
Centrally Acting Sympatholytics / Clonidine / α2 adrenceptor agonist / Hypertension / ↓ Sym outflow from Brain
Mononidine / Imadazoline agonist
Vasoconstrictor / Sumitriptan / 5HT1D agonist. Vasoconstriction of large arteries, inhibits trigeminal nerve transmission. / Migraine Attacks / Coronary vasoconstriction – do not use in patients with coronary disease.
Drugs of abuse / Cannabis / Inhalation 50%
Oral 10-15% ↑½-2hr duration t½=7days (remains in fat tissues). Metabolised in liver – active metabolite 11-hydroxy-THC. Enterohepatic cycling. 25% urine, 65% Bile / Endogenous cannabinoid receptors (hippocampus, cerebellum, cortex, basal ganglia CB1, immune cells CB2). Anandamide is endogenous agonist.
Inhibit GABA interneurones in VTA → disinhibition of dopaminergic projection. / Abuse / Effects on perception, depression of cognition, slow reaction times, defects in short term memory, ↑ satiety, motor incoordination / Tachycardia, vasodilation → reddening conjunctivae, postural hypotension and fainting, immunosuppressant, respiratory effects (tar, carcinogens), psychosis due to loss of anterior cingulated cortex → loss of inhibition and more primitive actions
Cocaine / IV. Oral. Nasal. Inhalation
t½=20-90min
Plasma/Liver Choliensterase / Ecgonine Methyl Ester, Benzoylecgonine
Inhibits reuptake of dopamine in NAcc / VC, ↑ Sym, ↑ HR, ↓ Cerebral Blood flow + hyper-pyrexia in CNS -> Epilsepy / Euphoria/Disphoria, Heightened Energy, Insomnia, Restlessness, Talkative, Violence, Anorexia
Nicotine / Inhalation 20% absorbed. Distributes rapidly in tissues. Elimination t½=2-3hrs. Metabolised in liver to cotinine. / Nicotinic receptor agonist. Sympathetic activation via peripheral receptors or directly on brain.
Binds to nicotinic receptors on dendrites of VTA neurones →↑ firing rate. / - / CVS: ↑Sym : ↑ HR, BP, SV, vasoconstriction, blood coagulation, LDL, VLDL, FFA, risk of atherosclerosis, MI, CVD, stroke. ↓ oxygen carrying capacity HDL
Metabolic: ↑metabolic rate, ACTH, cortisol, ↓appetite
Neurological:↓risk of Parkinson’s Alzheimer’s
Disulfiram / Acetaldehyde dehydrogenase inhibitor. Causes build up of acetaldehyde. / Aversion therapy for recovering alcoholics. / Acetaldehyde build up: flushing, tachycardia, panic, distress. / None when alcohol not present.
Drugs of abuse / Alcohol / Oral. 20% stomach, 80% SI. Substantial 1stPM – saturation kinetics. 90% metabolised, 10% excreted unchanged by lungs. 85% metabolised in liver, 15% Gut / ↑ GABA mediated inhibition (sedative effects)
Inhibition on Ca2+ entry →↓ NT release.
Inhibition of NMDA receptor function (memory loss?)
Major action on cortex, RAS, corpus callosum, hypothalamus, hippocampus, cerebellum, basal ganglia. / CNS: Depressant, ↓sensory function, concentration, motor function, reaction time, coordination. ↑confidence, euphoria, memory loss. Coma, resp failure. Dementia, degeneration of cerebellum, neuropathy, myopathy, Wernicke-Korsakoff syndrome.
CVS: Vasodilation, flushing, ↓Ca2+ entry, ↑prostaglandins, ↓thrombosis risk/ heart disease - ↑HDL, ↓plaque formation, ↓thromboxane, ↓platelet aggregation.
Chronic Liver: Fatty Liver -> Hepatitis -> Cirrhosis. Oesophageal Varice.
Endo: ↑ACTH, ↓Testosterone -> Feminisation.
Foetal Development.
Anticoagulants / Warfarin / Oral, absorbed quickly. Delayed Effect for 12-16hrs. t½=4-5days. 99.99% Plasma protein bound, hepatic metabolism by CYP450. / Inhibits the activation of vitamin K →Prevents synthesis of clotting factors II, VII, IX, X. / Prevention/ treatment of DVT, PE, prevent clotting during haemodialysis/ bypass surgery. / Anticoagulant / Haemorrhage, teratogenicity. Drug interactions with:
- Drugs inhibiting/ inducing CYP450
- Drugs which displace warfarin from albumin
- Drugs inhibiting platelet function
Heparin
LMWH / Poor oral absorption. Given S.C./ I.V. short t½. Saturation kinetics. LMWH has longer t½ and no saturation kinetics. / Activated antithrombin III which inhibits factor Xa and thrombin by active serine binding.
LMWH has less action on thrombin / Bleeding, thrombocytopenia, osteoporosis, hypersensitivity.
Reversal by protamine I.V., binds to give inactive complex.
Antiplatelet agents / Aspirin
(also NSAID) / Oral, highly plasma protein bound / Irreversible COX-1 (and slight COX-2) inhibitor. Acetylates active site. Prevents TXA2 and PGE2 production. / Prevention of high risk cardiovascular patients. Analgesic, antipyretic, anti-inflammatory / Analgesic, antipyretic, anti-inflammatory, antiplatelet. / GI sensitivity (ulceration, bleeding, perforation). ↓Creatinine clearance, ↑bleeding time, BronchoC
Clopidogrel / Oral. Peak plasma conc at 4hrs, effect delayed 4 days. / Pro-drug inhibits fibrinogen binding to GpIIb/IIIa receptors. / Aspirin sensitive patients / Prevents platelet aggregation / Bleeding, GI haemorrhage, diarrhoea, rash, rarely neutropenia.
Abciximab / I.V. Binds rapidly to platelets and cleared with platelets.
t½=24-48hrs. / Antagonist of GpIIb/IIIa receptor (monoclonal antibody) / Acute Coronary Syndromes, with heparin and aspirin to prevent ischaemia in unstable angina. / Bleeding, immunogenic.
Fibrinolytics / Streptokinase / I.V. 30-60 min infusion
t½=12-18mins / Binds to plasminogen and activates - conformational / Acute MI - ↓mortality (additive with aspirin), acute thrombotic stroke (3hrs), DVT, PE arterial thromboembolism / Break down clot / Bleeding, GI haemorrhage, stroke. Allergy
Alteplase / Recombinant tPA – works better on plasminogen bound to fibrin than soluble →clot sensitive. Activates Plasmin / Bleeding, GI haemorrhage, stroke. Not antigenic
Statins / Simvastatin
Pravastatin / Oral / HMG-CoA reductase inhibitors. ↓cholesterol production in the liver. ↑LDL receptors on hepatocytes →↓LDL in blood. / Patients with high cholesterol, blood pressure, diabetes or MI. / ↓Total cholesterol, LDL, TGs. ↑HDL / RARE: Myalgia, muscle cramps, myopathy, rhabdomyolysis, acute renal failure
Not for Pregenant Women.
Fibrate / Benzafibrate
Gemfibrozil / Ligand for PPAR-α -> ↑lipoprotein lipase activity / First Line for high TG / ↓10% LDL ↑10% HDL ↓30%TG
Misc / Nicotinic Acid / ↓VLDL release -> ↓ 30-50% TG. ↓ 10-20% Cholesterol + ↑HDL / A number of UE
Ezetimibe / Glucuronidation Activiated / Inhibits cholesterol absorption / Combination Therapy
Diuretics / Mannitol / Pharmacologically inert. Filtered by glomerulus, not reabsorbed. ↑osmolarity of tubular fluid →↓water reabsorption / Prevent acute renal failure (given in clinical setting due to ↑osmol) / ↑Urine volume / Electrolyte imbalance (hypernatraemia: nausea, vomiting, Pul Oe)↑ECF vol
Acetazolamine / Inhibit intra+extracellular carbonic anhydrase. ↓ HCO3 reabsorption →Na++H2O reabsorption ↓.↑Na+ delivery to DCT→↑K+ loss. / Used in glaucoma, metabolic alkalosis, renal stones. / ↑Urine volume, and ↑K+,Na+ and HCO3 excretion. / K+ loss, metabolic acidosis.
Frusemide
(Loop diuretic) / Oral, onset 1hr, DOA 4-6hrs. Tubular secretion, ~50% metabolised. / Inhibitor of Na+/2Cl-/K+ pump.
(Triple Transporter in Asc Limb). Dilutes interstitium →↓concentrating power of collecting duct. / Acute pulmonary oedema, oedema due to heart failure, renal or hepatic disease. Hypercalcaemia/ hyperkalaemia. / ↑Urine volume~15-30%, ↑Na+, K+, Cl-, Ca2+, Mg2+ excretion. / Metabolic alkalosis,
hypovolaemia,
hypotension,
hypokalaemia.
Bendrofluazide
(Thiazide) / Oral, onset 1-2hrs, DOA 8-12hrs. Tubular secretion. / Inhibitors of Na+/Cl- pump at DCT, →↑Na+ delivery to collecting duct →↓water reabsorption. ↑K+ loss due to compensation for Na+ / Congestive heart failure, hypertension, nephrogenic diabetes insipidus!?, severe resistant oedema. / ↑Urine volume 5-10%. ↑Na+,K+,Cl-,Mg2+ excretion. ↓Ca2+ excretion. / K+ loss, diabetes mellitus (interferes with insulin secretion), metabolic alkalosis.
Amiloride
(Potassium Sparing Diuretics) / Poor orally. Onset 6hrs. DOA 24hrs. Excreted unchanged. / Blocks Na+ channel in Na+/K+ exchange mechanism. ↑Na+ and ↓K+ loss. / With other diuretics to prevent K+ loss / ↑urine vol 5%. ↑Na+,H+, uric acid loss. / Hyperkalaemia, metabolic acidosis.
Spironolactone / Oral, onset/DOA – days. Filtered by glomerulus. / Aldosterone antagonist. Blocks Na+/K+ exchanger in DCT. ↑K+ retention. / Heart failure, hypertension to prevent K+ loss with diuretics. / ↑urine vol 5%. ↑Na+,H+, uric acid loss. / Hyperkalaemia, gynaecomastia, menstrual disorders, testicular atrophy.
Anti-emetics
(see also anti-muscarinics:
Hyoscine) / Promethazine / Oral. Onset in 1-2hrs, peak effect 4hrs, DOA 24hrs. / Competitive antagonist of H1>muscarinic>D2 receptors. Acts centrally at NST, vestibular nucleus and vomiting centres / Motion sickness, normally prophylactically. Disorders of labyrinth, morning sickness, pre-/post-operatively. / Also relief of allergic symptoms, anaphylaxis, night sedation. / Dizziness, tinnitus, fatigue, sedation (excitation in excess), convulsions, general anti-muscarinic.
Metoclopramide / Oral, rapid absorption, Extensive 1stPM. I.V. Crosses BBB and placenta. / Dopamine receptor antagonist (D2>H1>M). Acts centrally at CTZ. / Nausea & vomiting associated with toxins, e.g. uraemia, radiation sickness, GI disorders, chemotherapy. / ↑GI motility and gastric emptying. / Drowsiness, dizziness, extrapyrimidal reactions (children – Parkinsonian-like)
Hyperprolactinaemia.
anxiety, ↓bioavailability when co-administered.
Ondansetron / Oral, well absorbed, excreted in urine. / 5HT3 receptor antagonist. Blocks visceral afferents and CTZ. / Chemotherapy (cisplatin), radiation sickness and post-operatively. / Prevents nausea & vomiting associated with toxins and pain / Headache, flushing and warmth, constipation.
Gastric and duodenal ulcers / Antibiotics e.g. Metronidazole / Targets anaerobic bacteria and protozoa / Elimination of Helicobacter pylori as part of triple therapy. / Metronidazole interferes with alcohol metabolism
Amoxycillin / Broad spectrum
Clarithromycin / Inhibits bacterial tRNA translocation
Gastric and duodenal ulcers:
PPIs / Omeprazole / Oral. DOA 2-3days. Enteric coated for slow release. / Irreversible inhibitor of H+/K+ pump. Weak base that accumulates in canaliculi and is activated by acid. / Triple therapy for ulcers, GORD. / ↓acid secretion by 90% / Rare
H2 antagonists / Cimetidine / Oral, well absorbed. / Histamine receptor antagonists / Triple therapy for ulcers, GORD / ↓acid secretion by 60% / Rare. Likely relapse after withdrawal. CYP450 inhibitor
Ranitidine
Gastric and duodenal ulcers:
Cytoprotective drugs / Bismuth chelate / Strong negative charge in low pH. Binds to positive charge groups to form gel-like complex. Limits H+ and pepsin getting to ulcer. / Triple therapy, resistant cases / ↑PGs, mucus, HCO3 secretion. ↓ Helicobacter pylori / Constipation
↓Absorption of drugs and nutrients
Sucralfate
Misoprostal / PG agonist (analogue of PGE1) / Co-prescribed with oral NSAIDs / Maintains mucus barrier, ↓acid secretion / Diarrhoea, abdominal cramps, uterine contractions. Do not give in pregnancy
Ant-Acids / Ant-Acids
Al3+ & Mg2+ / Neutralises acid, ↑ gastric pH, ↓ Pepsin activity / Non-ulcer dyspepsia
Reduce duodenal ulcer
Respiratory Drugs
(Salbutamol & ipratropium) / Aminophylline / Oral, I.V. / Phosphodiesterase inhibitor. Prevents breakdown on cAMP → prolonged smooth muscle relaxation. / Asthma / Relaxation of airway smooth muscle.
Salmeterol / Long-acting 12hrs
Powder Inhalation / β2 receptor agonist / Asthma. COPD / Longer than Salbutamol
NSAIDs
(Aspirin) / Ibuprofen / Oral / Reversible COX-1 and COX-2 inhibitor. / Analgesic, anti-inflammatory, antipyretic / GI sensitivity (ulceration, bleeding, perforation). ↓Creatinine clearance, bronchoconstriction (lower incidence than aspirin)