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Year 2 - Theme A > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Simvastatin

A

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

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2
Q

Gemfibrozil

A

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

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3
Q

Acyclovir

A

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

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4
Q

Zidovudine

A

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

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5
Q

Amprenavir

A

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

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6
Q

Amphotericin/NYSTATIN

A

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

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7
Q

Fluconazole/ clotrimazole

A

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

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8
Q

Griseofulvin

A

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

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9
Q

Paclitaxel

A

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

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10
Q

Cisplatin

A

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

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11
Q

Salbutamol

A

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

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12
Q

Salmetrol

A

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

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13
Q

Theophylline

A

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

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14
Q

Montelukast

A

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

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15
Q

Ipratropium

A

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

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16
Q

Beclometasone

A

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

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17
Q

Methotrexate

A

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

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18
Q

Hydroxychloroquine

A

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

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19
Q

Azathioprine

A

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

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20
Q

Cyclophosphamide

A

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

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21
Q

Aspirin

A

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

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22
Q

Dipyridamole

A

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

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23
Q

Clopidogrel

A

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

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24
Q

Abciximab

A

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

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25
Q

Isoflurane

A

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

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26
Q

Nitrous Oxide

A

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

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27
Q

Propofol

A

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

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28
Q

Carbamazepine

A

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.

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29
Q

Phenytoin

A

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.

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30
Q

Ethosuximide

A

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

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31
Q

Valproate

A

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

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32
Q

Diazepam

A

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

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33
Q

Phenobarbital

A

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

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34
Q

Lamotrigine

A

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

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35
Q

Gabapentin

A

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

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36
Q

Captopril

A

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

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37
Q

Furosemide

A

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

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38
Q

Bendroflumethiazide

A

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

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39
Q

Spironalactone

A

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

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40
Q

Mannitol

A

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

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41
Q

Oxytocin

A

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

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42
Q

Pethidine

A

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

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43
Q

Paracetamol

A

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.

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44
Q

Amoxicillin

A

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

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45
Q

Benzylpenicillin

A

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

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46
Q

Flucloxacillin

A

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

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47
Q

Cefuroxime

A

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

48
Q

Ceftazidime

A

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

49
Q

Imipenem

A

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

50
Q

Vancomycin

A

GLYCOPEPTIDE ANTIBIOTIC

Actions: Bactericidal, interferes with cell wall synthesis in dividing bacteria

Use: MRSA infections, pseudomembranous colitis

SE: Reversible hearing loss, rarely: renal failure

51
Q

Doxycycline/ Tetracycline

A

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

52
Q

Gentamicin

A

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

53
Q

Erythromycin

A

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

54
Q

Clarithromycin

A

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

55
Q

Ciprofloxacin

A

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

56
Q

Sulfamethoxazole

A

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

57
Q

Trimethiprim

A

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.

58
Q

Isoniazid

A

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

59
Q

Rifampicin

A

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

60
Q

Pyrazinamide

A

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

61
Q

Ethambutol

A

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

62
Q

What is the treatment for TB?

A

Initial 2 months and 4 month continuation therapy:
Rifampicin and Isoniazid

Initial 2 months ONLY
Ethambutol and Pyrazinamide

63
Q

Quinine

A

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

64
Q

Pyrimethamine

A

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

65
Q

Artemether

A

ANTIMALARIAL

Actions: Blood schizonticide

MOA: Inhibits falciparum sarcoplasmic-endoplasmic reticulum calcium ATPase.

Use: uncomplicated falciparum malaria

SE: GIT disturbance, headache, dizziness, paraesthesia, myalgia, rash

66
Q

Atropine

A

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

67
Q

Pilocarpine

A

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

68
Q

Suxamethonium

A

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.

69
Q

Atracurium

A

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

70
Q

Atenolol

A

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

71
Q

Amphetamine

A

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

72
Q

Cocaine

A

SYMATHOMIMETIC

Actions: Inhibition of uptake of NA by uptake 1 leads to increased NA effects.

Use: Local anaesthetic

73
Q

Ibuprofen

A

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

74
Q

Celecoxib

A

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

75
Q

Sulfasalazine

A

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.

76
Q

Leflunomide

A

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

77
Q

Infliximab

A

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.

78
Q

Ciclosporin

A

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

79
Q

Prednisolone

A

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

80
Q

Disopyramide

A

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

81
Q

Lidocaine

A

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

82
Q

Flecainide

A

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.

83
Q

Amiodarone

A

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

84
Q

Propranolol

A

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.

85
Q

Verapamil

A

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

86
Q

Adenosine

A

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)

87
Q

Losartan

A

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

88
Q

Amlodipine

A

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

89
Q

Glyceryl trinitrate

A

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

90
Q

Digoxin

A

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

91
Q

Bromocriptine

A

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.

92
Q

Amantadine

A

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

93
Q

Donepezil

A

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

94
Q

Memantine

A

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

95
Q

Levodopa

A

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

96
Q

Selegiline

A

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.

97
Q

Fluorouracil

A

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

98
Q

Doxorubicin

A

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

99
Q

Imatinib

A

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

100
Q

Tamoxifen

A

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

101
Q

Amiloride

A

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

102
Q

Doxazosin

A

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

103
Q

Chlortalidone

A

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

104
Q

Warfarin

A

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

105
Q

Ethinylestrodiol

A

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

106
Q

Lithium

A

Action: mood stabiliser

MOA: ?interferes with membrane ion transport.

Use: bipolar, mania, depression

SE: diarrhoea, tremor, confusion, renal toxicity

107
Q

Ampicillin

A

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

108
Q

Testosterone

A

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

109
Q

Diclofenac

A

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

110
Q

Aurothiomalate

A

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

111
Q

Raloxifene

A

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

112
Q

Alendronate

A

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

113
Q

Calcitonin

A

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

114
Q

Fentanyl

A

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

115
Q

Diltiazem

A

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

116
Q

Budesonide

A

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

Year 2 - Theme A (7 decks)

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