Pharmacology Flashcards
Simvastatin
Action: HMG CoA reductase inhibitors (STATIN)
MOA: HMG is a precursor of cholesterol, therefore inhibits the formation of cholesterol by blocking the enzyme
Use: Lowering plasma cholesterol
SE: abnormalities in liver function, GIT disturbances
Gemfibrozil
Action: Fibrates, lipid lowering
MOA: Peroxisome proliferator-activated receptors (PPARs) act as transcription factors. They increase gene transcription and causes an increase in lipoprotein lipase leading to decreased TAG
Use: Hyperlipidaemia
SE: gall stones, GIT disturbances
Acyclovir
Action: DNA polymerase inhibitors
MOA: converts monophosphate to triphosphates. Inhibits viral DNA polymerase and terminates the nucleotide chain
Use: Herpes, hep C, cytomegalovirus
SE: minimal, renal dysfunction
Zidovudine
Action: nucleoside reverse transcriptase inhibitors
Virus uses reverse transcriptase to copy the viral single stranded RNA to DNA
MOA: blocks reverse transcriptase and prevents completion of synthesis into DNA and stops replication
Use: HIV and hep B
SE: GIT disturbance, headache, insomnia, neuropathy
Amprenavir
Action: protease inhibitor
MOA: Virus translates mRNA into inert polyproteins and the protease converts to proteins. Amprenavir blocks this.
Use: HIV (in combination)
SE: GIT disturbances, taste disturbance and sleep problems
Amphotericin/NYSTATIN
Action and MOA: Kills fungi by binding to the ergosterol in the fungal wall membrane (not found in our cell walls) and increasing membrane permeability
Use: Candidiasis, cryptococcal meningitis
SE: renal toxicity, GIT disturbances, neurological disturbances
Fluconazole/ clotrimazole
Action: fungistatic by inhibiting the synthesis of ergosterol that forms the cell wall
MOA: inhibits 14 alpha demethylase which is important in the coversion of lanosterol to ergosterol
SE: GI disturbances, headache, rash, hypersensitivity
Griseofulvin
Action: fungistatic by interfering with the mitosis of fungal cells
MOA: interacts with polymerised microtubules inhibiting spindle formation
Use: fungal infections of the skin, hair and scalp
SE: infrequent, GIT and headache
Paclitaxel
Actions and MOA: Binds to tubulin, keeping microtubules polymerised, preventing spindle formation in dividing cells and stopping mitosis
ADE: given by IV infusion
Use: non small cell lung cancer, ovary and breast cancer
SE: hypersenstivity reactions, myelosuppression, peripheral neuropathy, bradycardia, muscle & joint pain, hair loss, GI disturbance
Cisplatin
Actions and MOA: forms a reactive complex that causes intrastrand cross linking and denaturation of the DNA
ADE: IV infusion
Use: Cancer - lung, testes, ovaries, cervix, bladder, head and neck
SE: nephrotoxicity, ototoxicity, severe nausea and vomiting, myelosuppression, peripheral neuropathy
Salbutamol
SELECTIVE B2 AGONIST
Actions: bronchodilation, a physiological antagonist of spasmodic mediators
MOA: decreased calcium mediated contraction in bronchioles. Increased cAMP which activates protein kinase A (PKA). PKA inhibits myosin light chain kinase which is a mediator of contraction
Use: acute asthmatic attack. COPD. Prevent exercise induced asthma
SE: tremors, tachycardia, dysrhythmias
Salmetrol
LONG ACTING SELECTIVE B2 AGONIST
Actions: bronchodilation
MOA: decrease calcium mediated contraction in bronchioles. Increased cAMP, activates protein kinase A (PKA) which decreases myosin light chain kinase, which reduced contraction
Use: prevent bronchoconstriction with exercise induced asthma, or at night for those needing prolonged bronchodilator therapy. COPD
SE: tremros, tachycardia, dysrhythmias
Theophylline
XANTHINE
Actions: bronchodilation
MOA: Inhibits phosphodiesterase PDE4 thys increasing cAMP, relaxing smooth muscle. Inhibits PDE4 in inflammatory cells and decreases mediator release
Use: 2nd line for chronic asthma not controleed by B2 agonists
SE: GIT disturbance, tachycardia, anxiety
Montelukast
LEUKOTRIENE RECEPTOR ANTAGONIST
Actions: reverses brochoconstriction. Relaxes airway smotth muscle
MOA: Antagonist at cysteinyl leukotriene receptor on which bronchospasmic mediators LTc4, LTD4, LDE4 act. It decreases both early and late phase response
Use: 3rd line asthma treatment, used as adjunct to steroids and long acting B2
SE: few
Ipratropium
MUSCARINIC RECEPTOR ANTAGONIST
Actions: bronchodilation by inhibiting ACh mediated bronchoconstriction and mucus secretion
MOA: competitively antagonises ACh action on muscarinic receptors
Use: asthma adjunct to B2 agonists, steroids. COPD
SE: few
Beclometasone
ANTIASTHMATIC CORTICOSTEROID
Actions: reduces hyper-activity and decreases inflammatory delayed phase ONLY
MOA: reduces the activation of inflammatory cells and release of mediators especially chemokines
Use: added to bronchodilator therapy if inadequate
SE: hoarse voice, oral candidiasis
Methotrexate
DMARD
Action: Slows the appearance of new erosions in joints
MOA: folic acid analogue that inhibits purine and pyrimidine synthesis. It modulates secretion of cytokines and inhibits T cells
Use: Rheumatoid arthritis and cancer
Side effects: mucosal ulceration and nausea. Cirrhosis of the liver with chronic use.
NOTE: Requires periodic monitoring
Hydroxychloroquine
DMARD
MOA: Inhibition of phospholipase A2 and platelet aggregation, membrane stabilisation, antioxidant activity. They also have effects on the immune system that interferes with antigen processing
Use: RA
Side effects: ocular toxicity, irreversible retinal damage
Azathioprine
Action: immunosuppressive drug - purine analogue
MOA: It inhibits an enzyme required for DNA synthesis and affects proliferating cells e.g. T and B cells
Use: transplant rejection, rheumatoid arthritis, Crohn’s disease, ulcerative collitis
Side effects: nausea and vomiting, hypersensitivity, dizziness, fatigue, anaemia, acute pancreatitis
Cyclophosphamide
Action: bifunctional alkylating agent
MOA: cytotoxic effects on B and T cells. Selectively suppresses B lymphocyte activity. Modulates immune response
Use: cancer and autoimmune conditions
Side effects: increase risk of infection and bleeding. GI disturbances, alopecia, infertility, teratogenic, toxic to kidneys
Aspirin
Action: antiplatelet, analgesic
MOA: Irreversibly inactivates COX 1; alters balance between TXA2 and PGI2 in platelet/vascular endothelium axis
Use: Reduce risk of MI or TIA
Side effects: GI bleeding, bronchospasm
Dipyridamole
Action: Inhibitor of platelet aggregation
MOA: Phophodiesterase inhibitor. Has vasodilator activity; prevents platelet adenosine uptake and cyclic GMP phosphodiesterase action.
Use: secondary prevention of ischaemic stroke and TIA
Side effects: Headache, GIT disturbances and hypotension
Clopidogrel
Action: Prevents platelet aggregation/activation
MOA: Irreversibly inhibits the binding of ADP to the purine receptor on platelets inhibiting ADP mediated platelet aggreagation and interfering with Gp IIb/IIIa mediated platelet aggregation
Use: Prevention and treatment of MI
Side effects: Bleeding, GI discomfort, rashes
Abciximab
Action: Inhibits platelet aggregation
MOA: Monoclonal antibody Fab fragment against platelet GP IIb/IIIa receptor. binds and inactivates receptor preventing the binding of fibrinogen thus inhibiting aggregation
Use: Adjunct to heparin. Prevents restenosis and reinfarction
Side effects: Bleeding, thrombocytopaenia
Isoflurane
Action: CNS depressant. Causes unconsciousness. Weakly analgesic
MOA: Potentiates GABA action on GABA A receptors and opens K+ channels to reduce neuronal activity, especially in cerebral cortex, thalamus and hippocampus. Lipid solubility important for action
Use: maintenance and less frequently induction of general anaesthesia
Side effects: cardiac and respiratory depression. cardiac dysrhythmia. postop nausea and vomiting
Nitrous Oxide
Action: CNS depression, unconsciousness with anaesthetics, analgesia, euphoria
MOA: reduces opening of NMDA receptor channels. Increased opening of TREK potassium channels. Analgesic action inhibited by opioid antagonists suggesting release of endogenous opioids.
Use: general anaesthesia, must be combined by more potent agents
Side effects: Few. O2 may be required during recovery
Propofol
Action: ultrashort acting anaesthetic. Weak analgesic
MOA: Binds to particular site on GABA A receptor to enhance opening of intrinsic Cl- channel by GABA A.
Use: Anaesthesia for short procedures and induce anaesthesia.
Side effects: cardiorespiratory depression. postop vomiting
Carbamazepine
Action: Anticonvulsant - relieves neuropathic pain
MOA: Blocks Na+ channels to inhibit action potential and initiation and propagation. Use dependence of block means that action is preferentially on rapidly firing neurons in epileptic focus
Use: partial and general seizures (tonic clonic). Not absence. Status epilepticus. Neuropathic pain. bipolar disorder
Side effects: drowsiness, headache, mental disorientation, motor disturbances.
Phenytoin
Action: Anticonvulsant - relieves neuropathic pain
MOA: Blocks Na+ channels to inhibit action potential and initiation and propagation. Use dependence of block means that action is preferentially on rapidly firing neurons in epileptic focus
Use: partial and general seizures (tonic clonic). Not absence. Status epilepticus. Neuropathic pain. bipolar disorder
Side effects: drowsiness, headache, mental disorientation, motor disturbances.
Ethosuximide
Actions: Anticonvulsant, specific action on absence seizures
MOA: Blocks T type Ca2+ channels in thalamic neurons to counteract slow spike and wave firing pattern in absences
Use: absence seizures
SE: anorexia, GIT upset, pancytopaenia, rash, drowsiness, fatigue
Valproate
Actions: anticonvulsant. mood stabiliser
MOA: Block of voltage gated Na+ channels to inhibit action potential initiation and propagation; inhibition of GABA transaminase to reduce GABA breakdown, various effects on 2nd messenger pathways
Use: epilepsy especially myoclonic. manic bipolar. migraine
SE: nausea, vomiting, tremor, weight gain, teratogenic, hepatic and pancreatic toxicity
Diazepam
Actions: anticonvulsant. hypnotic and anxiolytic
MOA: interacts with benzodiazepine binding site on GABA A receptor to enhance channel opening by GABA. Increase Cl- permeability, decreased electrical excitability
Use: status epilepticus
SE: sedation. respiratory depression
Phenobarbital
Actions: anticonvulsant. hypnotic
MOA: binds to barbituate site on GABA A receptor to enhance activity of GABA in opening the CL- channel. decrease neuronal excitability and action potential frequency at epileptic focus. Effects on Na+ and Ca2+ channels
Use: tonic clonic and simple partial seizures
SE: sedation. megaloblastic anaemia, hypersensitivity and dependence
Lamotrigine
Actions: anticonvulsant. decrease frequency of episodes in bipolar disorder
MOA: inhibition of glutamate release decreases postsynaptic neuronal excitation. Na+ and possible Ca2+ channel inhibition
Use: partial and general seizures including absence. Bipolar disorder
SE: dizziness, headache, double vision, sedation
Gabapentin
Actions: anticonvulsant. analgesic
MOA: binding to units of Ca2+ channels to block entry and exocytosis of glutamate
Use: partial seizures. neuropathic pain
SE: sedation, dizziness, unsteadiness
Captopril
Actions: lowers BP by decreasing vasoconstrictor tone. Affect capacitance and resistance vessels and reduce cardiac load and arterial pressure
MOA: inhibits angiotensin-converting enzyme reducing synthesis of vasoconstrictor angiotensin II and decreasing aldosterone secretion
Use: hypertension, cardiac failure, following MI, progressive renal insufficiency, diabetic neuropathy
SE: hypotension, dry cough, angioedema, renal failure
Furosemide
DIURETIC - LOOP
Actions:causes copious urine production by inhibiting NaCl reabsorption in the thick ascending look of Henle. Increase Ca2+.
MOA: Inhibits Na+/K+/2Cl- cotransporter in luminal membrane by binding with the chlorine binding site
Use: pulmonary oedema, chronic heart failure, ascites, hypercalcaemia, hyperkalaemia
SE: hypokalaemic alkalosis, hypovolaemia, hypertension
Bendroflumethiazide
THIAZIDE DIURETIC
Actions: causes moderate diuresis by inhibiting NaCl reabsorption in the distal tubule. Increased K+ and H+ secretion. Decreased Ca2+ and uric acid excretion. Increased Mg2+ excretion. Some vasodilator action
MOA: inhibits Na+/Cl- cotransporter in the luminal membrane of the distal convoluted tubule
Use: hypertension, mild heart failure, kidney stones, nephrogenic diabetes insipidus
SE: K+ loss, metabolic acidosis, hyperuricaemia, increased insulin requirement, erectile dysfunction
Spironalactone
K+ SPARING DUIRETIC
Actions: Inhibits Na+ reabsorption in distal nephron. Decreased K+ excretion
MOA: Competitve antagonist of aldosterone, prevents production of aldosterone mediator that normally causes Na+ influx by activating Na+ channel in collecting tubule
Use: hypertension, primary and secondary hyperaldosteronism
SE: hyperkalaemia and gynaecomastia
Mannitol
OSMOTIC DIURETIC
Actions: increased water excreted by the kidneys
MOA: passes into filtrate at glomerulus and no resorbed. Acts in those that are freely permeable to water
Use: cerebral oedema and increased intraocular pressure
SE: temporary expansion of extracellular fluid compartment. Pulmonary oedema
Oxytocin
Actions: contract the uterus causing coordinated contractions that travel from the fundus to cervix with complete relaxation between contractions. Vasodilator action
MOA: acts on oxytocin receptors in myometrium
Use: induce labour, prevent post partum delivery
SE: hypotension, water retention
Pethidine
OPIOID RECEPTOR AGONIST
Actions: analgesia
MOA: activates mu opioid receptors to inhibit pain transmission
Use: moderate-severe pain. Favoured for labour pain as does not reduce uterine contractions
SE: constipation, nausea, vomiting
Paracetamol
NSAID
Actions: analgesia. antipyretic. little anti-inflammatory action
MOA: Inhibition of COX1 and 2
Use: mild to moderate pain, especially headache.
SE: few. nausea and vomiting with high dose.
Amoxicillin
BROAD SPEC ANTIBIOTIC
Actions: Bactericidal; interferes with cell wall synthesis in dividing bacteria
MOA: Binds to and inhibits the enzyme that cross links the peptide chain of the newly formed building blocks to the peptidoglycan cell wall backbone
Use: Gram negative bacteria as well as streptococcal, gonococcal, meningococcal infections, anthrax, diptheria, gas gangrene
SE: hypersensitivity, GIT distrubance
NOTE: inactivated by bacterial beta lactamases
Benzylpenicillin
BETA LACTAM ANTIBACTERIAL AGENT
Actions: Bactericidal; interferes with cell wall synthesis in dividing bacteria
MOA: Binds to and inhibits the enzyme that cross-links the peptide chain of the newly formed building block to the peptidoglycan cell wall backbone
Use: streptococcal, gonococcal, menigococcal, anthrax, diptheria, gas gangrene
SE: hypersensitivity reactions
NOTE: inactivated by beta lactamases
Flucloxacillin
BETA LACTMASE-RESISTANT PENICILLIN ANTIBACTERIAL AGENT
Actions: bactericidal, interferes with cell wall synthesis in dividing bacteria
MOA: binds to and inhibits the enzyme that cross-links the peptide chain of newly formed building blocks to the peptidoglycan wall backbone
Use: penicillin resistant staphylococci infections
SE: hypersensitivity reactions, GIT disturbances
Cefuroxime
2ND GEN CEPHALOSPORIN BETA LACTAM ANTIBIOTIC
Actions: Bactericidal; interferes with cell wall synthesis in dividing bacteria
MOA: Binds to and inhibits the enzyme that cross-links the peptide chain of the newly formed building blocks to the peptidoglycan cell wall backbone
Use: Active against beta lactamase producing bacteria (H.influenza, N.gonorrhoea) Sinusitis, ear infections, lower respiratory tract infections, UTI
SE: hypersensitivity reactions, GIT disturbance, colitis, superinfection
Ceftazidime
3RD GEN CEPHALOSPORIN BETA LACTAM ANTIBIOTIC
Actions: bactericidal; interferes with cell wall synthesis in dividing bacteria
MOA: Binds to and inhibits the enzyme that cross-links the peptide chain of the newly formed building blocks to the peptidoglycan cell wall backbone
Use: Gram positive and gram negative
SE: hypersensitivity, GIT disturbance, colitis, superinfection
Imipenem
CARBAPENEM BETA LACTAM ANTIBIOTIC
Actions: Bactericidal; interferes with cell wall synthesis in dividing bacteria
MOA: Binds to and inhibits the enzyme that cross links the peptide chain of the newly formed building blocks to the peptidoglycan cell wall backbone
Use: Broad spec. Gram positive and negative as well as anaerobic bacteria.
SE: GIT disturbance, rashes, injection site reaction
Vancomycin
GLYCOPEPTIDE ANTIBIOTIC
Actions: Bactericidal, interferes with cell wall synthesis in dividing bacteria
Use: MRSA infections, pseudomembranous colitis
SE: Reversible hearing loss, rarely: renal failure
Doxycycline/ Tetracycline
BROAD SPEC TETRACYCLINE ANTIBIOTIC
Actions: Interferes with bacterial protein synthesis by competing the tRNA for the A site of the ribosome and reversibly inhibiting its binding to the mRNA codons in the 30s subunit
Use: chlamydial, rickettsial and brucella infections. H.influenza, mycoplasma. Sinusitis, prosratitis, syphilis, lyme disease and prevention and treatment of malaria
SE: staining of the teeth, GIT disturbance, anorexia, flushing, tinnitus
Gentamicin
BACTERIAL AMINOGLYCOSIDE ANTIBIOTIC
Actions: Inhibits bacterial protein synthesis
MOA: Causes misreading of the mRNA message due to abnormal codon:anticodon recognition with the production of abnormal proteins
Use: Infections with staphylococci, streptococci, enterococci, gram negative bacilli. Septicaemia, meningitis, pyelonephritis, endocarditis, pneumonia
SE: dose related ototoxicity and nephrotoxicity. GIT disturbance, rash, blood disorders
Erythromycin
MACROLIDE ANTIBIOTIC
Actions: Inhibits bacterial protein synthesis
MOA: Inhibits the translocation of the transfer RNA from the A site to the P site
Use: pneumococcal and streptococcal infections for those allergic to penicillin. Chlamydial and mycoplasma infections. Skin and respiratory tract infections. syphilis, diptheria, prostatisis, whooping cough, campylobacter enteritis
SE: GIT disturbances. Less frequent - allergic reaction and cholestatic jaundice
Clarithromycin
MACROLIDE ANTIBIOTIC
Actions: Inhibits bacterial protein synthesis
MOA: Inhibits the translocation of the transfer RNA from the A site to the P site
Use: pneumococcal and streptococcal infections for those allergic to penicillin. Chlamydial and mycoplasma infections. Skin and respiratory tract infections. syphilis, diptheria, prostatisis, whooping cough, campylobacter enteritis
SE: GIT disturbances. Less frequent - allergic reaction and cholestatic jaundice
Ciprofloxacin
BACTERIAL FLUOROQUINOLONE
Actions: Interferes with bacterial DNA function
MOA: Inhibits DNA gyrase (topoisomerase II) - the enzyme that produces the supercoil in the chromosome that is essential for transcription and replication
Use: Gram positive and negative. UTI, GIT, bone and joint infections.
SE: GIT upsets, headache, dizziness, rashes. Rare - tendon damage, CNS effects
Sulfamethoxazole
Actions: Interfere with bacterial folate metabolism and thus DNA synthesis
MOA: Competitively inhibits the enzyme dihydropteroate synthase. Stops conversion from PABA to folate.
Use: (with trimethiprim) pneumocystitis pneumonia, toxoplasmosis, nocardiasis, UTI, chronic bronchitis exacerbations.
SE: GIT upsets, rashes,. Very rare but serious: Stevens-Johnson syndrome, blood dyscrasias
Trimethiprim
Actions: Interferes with bacterial folate metabolism and thus DNA synthesis
MOA: Inhibits dihydrofolate reductase and thus the conversion of folate to tetrahydrofolate
Use: (with sulfamethoxazole) pneumocystis pneumonia, toxoplasmosis, nocardiasis, UTI, chronic bronchitis exacerbations. Used alone for: prostatisis, UTI, RTI
SE: GIT upsets, rashes.
Isoniazid
ANTI TB DRUG
Actions: bacteriostatis for resting mycobacteria, bactericidal for proliferating mycobacteria
MOA: disrupts the synthesis of mycolic acids - major components of mycobacterial cell walls
Use: TB
SE: GIT disturbance, hypersensitivity, peripheral neuritis
Rifampicin
ANTI TB DRUG
Actions: Bactericidal for mycobacteria; also effective against more Gram positive and negative bacteria
MOA: inhibits bacterial but not human DNA-dependent RNA polymerase leading to reduced RNA synthesis in the cell wall
Use: TB. Leprosy. Prophylaxis for H.influenzae and meningococcal meningitis.
SE: GIT disturbance, hepatitis, rash, orange salivia, sweat and tears.
NOTE: decreases action of anti-coagulants, narcotic analgesics, phenytoin, glucocorticoids and oral contraceptives
Pyrazinamide
ANTI TB DRUG
Actions: Bactericidal for actively dividing intracellular mycobacteria. Main effects occur in first few months
MOA: Is converted to pyrazinoic acid which disrupts membrane energetics and inhibits membrane transport function in mycobacterium tuberculosis
Use: TB
SE: joint pain, GIT disturbance, sideroblastic anaemia, rash
NOTE: decreases action of anti-coagulants, narcotic analgesics, phenytoin, glucocorticoids and oral contraceptives
Ethambutol
ANTI TB DRUG
Actions: Bacteriostatic for rapidly growing TB bacilli
MOA: It obstructs the formation of the cellw all in dividing TB bacilli
Use: TB
SE: visual disturbances (colour blind/loss of acuity), peripheral neuritis, rash, fever
What is the treatment for TB?
Initial 2 months and 4 month continuation therapy:
Rifampicin and Isoniazid
Initial 2 months ONLY
Ethambutol and Pyrazinamide
Quinine
ANTIMALARIAL
Actions: schizonticidal drug that kills malarial parasites in red blood cells
MOA: It is thought to inhibit haem polymerase which would normally degrade haem, rendering it harmless to the parasite. The toxic haem molecules accumulate and kill the parasite
Use: acute attacks of malaria
SE: GIT disturbance, tinnitus, blurred vision
Pyrimethamine
ANTIMALARIAL
Actions: A slow blood schizonticide
MOA: Inhibits the malaria parasites dihydrofolate reductase (DHFR) and interferes with its thymidylate synthesis.
Use: falciparum malaria
SE: GIT disturbance, depression of haemopoiesis, rashes, allergic alveolitis
Artemether
ANTIMALARIAL
Actions: Blood schizonticide
MOA: Inhibits falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase.
Use: uncomplicated falciparum malaria
SE: GIT disturbance, headache, dizziness, paraesthesia, myalgia, rash
Atropine
MUSCARINIC RECEPTOR ANTAGONIST
Actions: Inhibits secretions. Tachycardia. Relaxes smooth muscle. Anti-emetic
MOA: Competitive reversible antagonism at all muscarinic receptors
Use: Paralysis of accommodation and pupil dilation for eye examination (tropicamide). Urinary incontinence (oxybutinin), irritable bowel syndrome (dicylcoverine). Antidote for anticholinesterase poisoning. Treatment of cardiac slowing
SE: constipation, hyperthermia, dry mouth, urinary retention, blurred vision, raised intraocular pressure, CNS excitment
Pilocarpine
MUSCARINIC RECEPTOR AGONIST
Actions: Parasympathetic actions: contracts smooth muscle, decreases rate and force of heart beat; glandular secretion; inhibits neurotransmitter release
MOA: Action in glaucoma is due to interaction with M3 receptors which couple to Gq to increase cellular IP3 and DAG concentrations. Constriction of pupil aids drainage of aqueous humor and lowers intraocular pressure
Use: Glaucoma.
SE: Blurred vision
Suxamethonium
NICOTINIC RECEPTOR AGONIST - DEPOLARISING NEUROMUSCULAR BLOCKER
Actions: short lasting paralysis of skeletal muscle
MOA: action on nicotinic receptors produces a maintained depolarisation of the muscle membrane. This inactivates Na+ channels which propagate the action potential throughout the muscle. Action potential fails to spread and prevents muscle contraction in response to motor nerve activity
Use: short last paralysis to aid tracheal intubation and for short operative procedures
SE: hyperkalaemia, hypotension, bradycardia, muscle pain, raised intraocular pressure.
Atracurium
NICOTINC RECEPTOR ANTAGONIST - NON DEPOLARISING NEUROMUSCULAR BLOCKER
Actions: paralysis of skeletal muscle
MOA: reversible competitve antagonism at muscle type nicotinic receptors. inhibits binding of ACh to the receptors at the muscle end plate. End plate potential fails to reach threshold for propagation of the action potential along the muscle fibre. Reversed by AChE
Use: general anaesthesia to aid tracheal intubation
SE: minimal
Atenolol
BETA 1 ANTAGONIST
Actions: Reduces BP - decreases CO, renin and sympathetics. In angina it slows the heart and reduces metabolic demand
MOA: Block of the action of endogenous and exogenous agonists on B1 receptors
Use: Hypertension. Angina. Prevention of dysrhythmia in MI
SE: Bronchoconstriction in asthma, emphysema; potential heart block or heart failure in patients with coronary heart disease; decreased sympathetic warning to hypoglycaemia
NOTE: water soluble, can cause nightmares
Amphetamine
SYMPATHOMIMETIC
Actions: Release NA from the varicosity and has similar actions to NA and adrenaline.
alpha1 = vasocontriction = increased BP
beta 1 = increased HR
beta 2= bronchodilation
MOA: Taken up by uptake 1 into the varicosity, then into the vesicle by exchange with NA; the NA now loose in the cytoplasm, is then released by exchange with amfetamine at uptake 1
Use: narcolepsy, hyperactivity in children
SE: increased BP, tachycardia. insomnia, psychosis
Cocaine
SYMATHOMIMETIC
Actions: Inhibition of uptake of NA by uptake 1 leads to increased NA effects.
Use: Local anaesthetic
Ibuprofen
NSAID
Actions: Reduces inflammation, is analgesic for inflammatory pain, is antipyretic
MOA: reversible inhibition of COX 1, weak inhibition of COX2
Use: inflammatory conditions, dysmenorrhoea
SE: GI disturbance - gastric bleeding, headache, dizziness, allergic reaction
Celecoxib
Coxib NSAID
Actions: analgesic, antipyretic, anti-inflammatory. NO antiplatelet action
MOA: selective inhibition of COX2.
Use: RA, OA, ankylosing spondylitis
SE: fewer GI problems than normal NSAIDS. Renal toxicity
Sulfasalazine
DMARD
Actions: produces remission of RA, disease progression reduced
MOA: In the colon the salicylic acid moiety is released, is absorbed and has anti-inflammatory action
Use: RA, juvenile arthritis, IBS
SE: nausea, vomiting, headaches, rashes.
Leflunomide
DMARD
Actions: modifies the immune reaction underlying RA through an inhibitory action on activated T cells
MOA: Gives rise to a metabolite that inhibits dihydroorate dehydrogenase; inhibition of T cell proliferation and decreased producton of autoantibodies by B cells
Use: RA
SE: 25% get diarrhoea, increased BP, weight gain
Infliximab
ANTICYTOKINE ANTIRHEUMATIC DRUG
Actions: reduces joint inflammation and symptoms of RA. Reduces symptoms of Crohn’s disease
MOA: monoclonal antibody against TNF alpha that binds with the TNF alpha and prevents its interaction with cell surface receptors in inflammatory cells
Use: active RA. ankylosing spondylitis, psoriatic arthritis
SE: nausea, vomiting, headache, upper RTI.
Ciclosporin
IMMUNOSUPPRESSANT
Actions: Reduces cell mediated immune response; lesser effect on antibody mediated responses. Interferes with antigen induced T cell differentiation and the clonal proliferation of T cells and thus the development and activation of cytotoxic T cells
MOA: Complexes with cyclophilin to inhibit calcineurin which normally activates the transcription of IL2
Use: Organ rejection, preventing graft v host disease. Autoimmune disease
SE: nephrotoxicity, hypertension, hepatotoxicity, GIT disturbances
Prednisolone
GLUCOCORTICOID
Actions: Inhibits clonal proliferation of T and B cells and macrophage activation
MOA: interact with intracellular receptors to inhibit the transcription of specific genes that code for various cytokines (IL2)
Use: transplant rejection, inflammatory condition
SE: suppression of response to infection and endogenous GC synthesis. Osteoporosis, growth suppression in children, Cushings syndrome
Disopyramide
Class 1a antidysrhythmic
Actions: antidysrhythmic
MOA: Blocks open and inactivated Na+ channels in the cell membrane to reduce the rate of phase 0 depolarisation thus causes an increase in the refractory period and slowed AV production
Use: Supraventricular and ventricular dysrhythmia
SE: atropine like effects - blurred vision, dry mouth, constipation, urinary retention
Lidocaine
CLASS 1B ANTIDYSRHYTHMIC
Actions: antidysrhythmic, local anaesthetic
MOA: Blocks open and inactivated Na+ channels in the cell membrane. Na+ channel block reduces the rate of phase 0 depolarisation, increasing effective refractory period and slowing AV production
Use: Treatment and prevention of ventricular fibrillation especially following infarction. Digoxin induced arrythmias
SE: drowsiness, tremors, convulsions
Flecainide
CLASS 1C ANTIDYSRHYTHMIC
MOA: Preferential block of open Na+ channels. Reduces rate of phase 0 depolarisation causing an increase in the effective refractory period and slowed AV conduction
Use: prevention of paroxysmal atrial fibrillation. Severe ventricular dysrhythmia
SE: increased likelihood of dysrhythmia. Increase mortality due to ventricular fibrillation post infarction.
Amiodarone
ANTIDYSRHYTHMIC - class 3
MOA: Block K+ channels in the membrane to delay repolarisation and increase action potential duration. Increases refractory period. Also blocks Na+ channels
Use: Most effective. AF and flutter, ventricular ectopic beats and tachyarrhymias
SE: torsades de pointe. Pulmonary fibrosis, liver damage, skin rashes, thyroid malfunction
Propranolol
CLASS 2 ANTIDYSRHYTMIC
Actions: also Beta blocker
MOA: blocks sympathetic drive reducing pacemaker activity (phase 4) and increasing AV conduction time. Reduces the slow inward Ca2+ current which affects phase 2 of the action potential
Use: Reduction of mortality after infarct. Paroxysmal AF.
SE: Bronchoconstriction in asthmatics. Cardiac slowing.
Verapamil
CLASS 4 ANTIDYSRHYTHMIC
Actions: Antidysrhythmic. Blocks Ca2+ channels in cardiac and smooth muscle so has both negative inotropic and smooth muscle relaxant actions
MOA: Blocks L type voltage gated Ca2+ channels which are important in the action potential plateau and in particular affects action potential propagation in the SA and AV nodes. Decreased automaticity and slows AV conduction
Use: Supraventricular tachycardias. Control of ventricular rate in AF
SE:hypotension, dizziness, ankle oedema, constipation
Adenosine
ANTIDYSRHYTHMIC
MOA: Activates GPCR (adenosine). Inhibition of Ca2+ channel opening and increased K+ opening. Negative chronotropic action on SA node and slowed AV conduction
Use: termination of paroxysmal supraventricular tachycardia
SE: flushing, chest pain, dyspnoea, bronchospasm (all short lived)
Losartan
ANGIOTENSIN RECEPTOR ANTAGONIST
Actions: Lowers BP by decreasing vasoconstrictor tone
MOA: Blocks the action of angiotensin II on the angiotensin II (AT1) receptor
Use: hypertension, congestive heart failure, nephropathy
SE: hypotension, dizziness, hyperkalaemia
Amlodipine
CALCIUM CHANNEL BLOCKER
Actions: vascular dilation lowers BP.
MOA: Block voltage gated calcium channels in vascular smooth muscle inhibiting calcium influx and thus contraction
Use: hypertension, angina
SE: reflex tachycardia, hypotension, headache
Glyceryl trinitrate
VASODILATOR
Actions: dilates and relaxes vascular smooth muscle and thus reduce cardiac work and therefore metabolic demand, increase perfusion and oxygenation of heart muscle
MOA: gives rise to NO in the cell wall which activates protein kinase G (PKG) and reduces contraction
Use: angina (stable and unstable)
SE: headache due to vasodilation, postural hypotension
Digoxin
CARDIAC STIMULANT
Actions: slows heart. slows AV conduction. Prolongs AV node refractory period. Increases contraction in failing heart
MOA: inhibits Na+/K+ ATPase in plasma membrane. Increased intracellular Na+ reduces Ca2+ extrusion thus increasing calcium
Use: AF, heart failure
SE: dysrhythmias, yellow vision, nausea, vomiting
Bromocriptine
DOPAMINE RECEPTOR AGONIST
Actions: Antiparkinsonian. Inhibits prolactin secretion from pituitary
MOA: Activation of D2 receptors on striatal neurones counters impairment of dopaminergic transmission. Actions on D1 receptors may be important in ameliorating the non-Parkinsons symptoms associated with disease
Use: Parkinson’s. Amenorrhoea, acromegaly
SE: hallucinations, sleepiness, postural hypotension.
Amantadine
ANTIVIRAL AND PARKINSON’S TREATMENT
Actions: Antiparkinsonian, antiviral
MOA: Increasing dopamine release from nerve endings in striatum. Antimuscarininc actions
Use: Parkinson’s.
SE: Nausea, dizziness, insomnia, postural hypotension
Donepezil
ANTICHOLINESTERASE - CENTRAL ACTING
Actions: ameliorates symptoms of Alzheimers
MOA: reversible inhibition of acetylcholinesterase. Enhances cholinergic transmission in the cerebral cortex and hippocampus
Use: mild to moderate Alzheimer’s, limited relief of symptoms
SE: nausea, diarrhoea, vomiting, bradycardia, increased gastric acid secretion
Memantine
NMDA RECPTOR ANTAGONIST
Actions: Ameliorates symptoms of Alzheimer’s disease
MOA: open channel block of NMDA receptors. Prevents Na+ and Ca2+ entry into the neurone, so reducing glutamate excitotoxicity.
Use: moderate to severe Alzheimer’s. Only symptomatic relief
SE: well tolerated. confusion, dizziness, headache, insomnia, agitation, hallucinations
Levodopa
DOPAMINE PRECURSOR
Actions: Antiparkinsonian
MOA: Decarboxylation of levodopa to dopamine restores some activity in nigrostriatal activity.
Use: Parkinson’s. More effective against akinesia and rigidity than tremor
SE: anorexia, nausea, vomiting, postural hypotension. Acute schizophrenia-like syndrome
Selegiline
MAOB inhibitor
Actions: Antiparkinsonian
MOA: selective irreversible inhibition of MAOB, the isozyme which has dopamine as a preferred substrate. Potentiates action of endogenous dopamine and dopamine administered as levadopa
Use: Parkinson’s. Major depression
SE: nausea, dyskinesia. depression, insomnia, postural hypotension, hallucinations, confusion.
Fluorouracil
ANTIMETABOLITE ANTICANCER DRUG
Actions: Interferes with the synthesis if dTMP and thus with DNA synthesis
MOA: Gives rise to a fraudulent nucleotide and inhibits thymidylate synthase
Use: Cancer - GIT, pancreas, breast, malignant skin conditions
SE: myelosuppression, GIT disturbances, mucositis
Doxorubicin
CYTOTOXIC ANTICANCER DRUG
Actions: Inhibits DNA and RNA synthesis through an effect on topoisomerase II
Use: acute leukaemias, Hodgkin, non-Hodgkin lymphoma, tumours of breast, ovary, bladder, bronchi
SE: nausea, vomiting, cardiac damage, myelosuppression, hair loss
Imatinib
ANTICANCER PROTEIN KINASE INHIBITOR
Actions: Inhibits protein kinases in chronic myeloid leukemia and other malignancies
Use: CML, ALL, GIT stromal tumours, chronic eosinophilic leukaemia
SE: GIT disturbance, abdominal pain, oedema, haemorrhage, cough, dyspnoea, paraesthesia
Tamoxifen
OESTROGEN RECEPTOR AGONIST
Actions: Competes with endogenous oestrogen for the oestrogen receptor, preventing cell activation and proliferation
Use: Breast cancer
SE: Hot flushes, GIT disturbance, headache, menstrual irregularities
Amiloride
POTASSIUM SPARING DIURETIC
Actions: Inhibits sodium reabsorption in the distal nephron. Reduces K+ excretion
MOA: inhibits the sodium channel in the luminal membrane of the collecting tubule, reducing sodium influx
Use: Given with K+ losing diuretics to limit K+ loss
SE: hyperkalaemia, acidosis
Doxazosin
ALPHA 1 RECEPTOR ANTAGONIST
Actions: Vasodilation and decreased BP. Increased HR, decreases bladder sphincter tone. Inhibition of hypertrophy of smooth muscle in the bladder neck and prostate
MOA: block the action of endogenous and exogenous agonists on alpha 1 receptors
Use: severe hypotension, BPH
SE: dizziness, hypotension, headache, priaprism
Chlortalidone
THIAZIDE DIURETIC
Actions: causes moderate diuresis by inhibiting NaCl reabsorption in the distal tubule. Increased K+ and H+ secretion. Decreased Ca2+ and uric acid excretion. Increased Mg2+ excretion. Some vasodilator action
MOA: inhibits Na+/Cl- cotransporter in the luminal membrane of the distal convoluted tubule
Use: hypertension, mild heart failure, kidney stones, nephrogenic diabetes insipidus
SE: K+ loss, metabolic acidosis, hyperuricaemia, increased insulin requirement, erectile dysfunction
Warfarin
ANTICOAGULANT
Action: inhibits blood coagulation
MOA: Inhibits the reduction of vit K and thus prevents the gamma carboxylation of the glutamate residues in factor 2,7,9,10.
Use: treat DVT, PE. AF.
SE: Bleeding, treated with vit K
Note: monitor PTT
Ethinylestrodiol
ORAL CONTRACEPTIVE
Action: Prevention of pregnancy
MOA: suppresses the development of ovarian follicle by inhibiting FSH release from ant. pituitary.
SE: weight gain, flushing, mood changes, dizziness, acne
Lithium
Action: mood stabiliser
MOA: ?interferes with membrane ion transport.
Use: bipolar, mania, depression
SE: diarrhoea, tremor, confusion, renal toxicity
Ampicillin
BROAD SPEC ANTIBIOTIC
Actions: Bactericidal; interferes with cell wall synthesis in dividing bacteria
MOA: Binds to and inhibits the enzyme that cross links the peptide chain of the newly formed building blocks to the peptidoglycan cell wall backbone
Use: Gram negative bacteria as well as streptococcal, gonococcal, meningococcal infections, anthrax, diptheria, gas gangrene
SE: hypersensitivity, GIT distrubance
NOTE: inactivated by bacterial beta lactamases
Testosterone
Actions: as endogenous
MOA: converted to dihydrotestosterone which enters cells and interacts with nuclear receptors to initiate transcription of some genes and represion of others
Use: replacement therapy in hypogonadism
SE: infertility (eventually), oedema
Diclofenac
NSAID
Actions: Reduces inflammation, is analgesic for inflammatory pain, is antipyretic
MOA: reversible inhibition of COX 1, weak inhibition of COX2
Use: inflammatory conditions, dysmenorrhoea
SE: GI disturbance - gastric bleeding, headache, dizziness, allergic reaction
Aurothiomalate
GOLD COMPOUND
Action: reduces joint inflammation
MOA: Inhibits the erosion of cartilage and bone within the joint by inhibiting the synthesis of prostaglandins and modulates phagocytic cells
Use: RA
SE: dyspepsia, nausea, vomiting, flushing, headache
Raloxifene
SERM
Actions: It has agonist effects on bone and on the CVS but antagonist action on mammary glands and the uterus
MOA: like the oestrogens, it inhibits the cytokines that recruit osteoclasts
Use: Prophylaxis for postmenopausal osteoporosis and breast cancer
SE: risk of thromboembolism
Alendronate
BISPHOSPHONATE
Actions: decreases bone resorption and increase bone density
MOA: It prevents osteoclast mediated bone resorption. Incorporated into bone matrix and ingested by osteoclasts, promoting osteoclast apoptosis
Use: Postmenopausal osteoporosis, Paget’s, hypercalcaemia, bone secondaries in breast cancer
SE: GIT disturbances particularly in oesophagitis, bone pain, osteonecrosis of the jaw
Calcitonin
Actions: lowers serum calcium levels and decreases bone resorption
MOA: it decreases the reabsorption of both calcium and phosphate in the kidney; it inhibits bone resorption by binding to a specific receptor on osteoclasts, inhibiting their action
Use: hypercalcaemia; Paget’s disease; the prevention of postmenopausal osteoporosis
SEL GIT disorders; facial flushing; taste disturbances; dizziness; muscle pain
Fentanyl
OPIOID RECEPTOR AGONIST
Actions: analgesia
MOA: activates mu opioid receptors to inhibit pain transmission
Use: moderate-severe pain. Favoured for labour pain as does not reduce uterine contractions
SE: constipation, nausea, vomiting
Diltiazem
CALCIUM CHANNEL BLOCKER
Actions: vascular dilation lowers BP.
MOA: Block voltage gated calcium channels in vascular smooth muscle inhibiting calcium influx and thus contraction
Use: hypertension, angina
SE: reflex tachycardia, hypotension, headache
Budesonide
ANTIASTHMATIC CORTICOSTEROID
Actions: reduces hyper-activity and decreases inflammatory delayed phase ONLY
MOA: reduces the activation of inflammatory cells and release of mediators especially chemokines
Use: added to bronchodilator therapy if inadequate
SE: hoarse voice, oral candidiasis
