PPT Flashcards
Amitriptyline
TRICYCLIC ANTIDEPRESSANT
Actions: antidepressant, neuropathic pain
MOA: Inhibits reuptake of NA and 5HT3 into neurons, increasing transmitter actions
Use: depression, panic disorder, neuropathic pain. enuresis
Side effects: sedation, blurred vision, dry mouth, constipation, urinary retention
- Overdose potentially fatal due to cardiac dysrhythmia, severe hypotension, seizure and CNS depression
- Increased risk of suicide in younger patients
- Clinical effects not seen for a few weeks
Imipramine
TRICYCLIC ANTIDEPRESSANT
Actions: antidepressant
MOA: Inhibits reuptake of NA and 5HT3 into neurons, increasing transmitter actions
Use: depression, panic disorder, neuropathic pain. enuresis
Side effects: sedation, blurred vision, dry mouth, constipation, urinary retention
- Overdose potentially fatal due to cardiac dysrhythmia, severe hypotension, seizure and CNS depression
- Increased risk of suicide in younger patients
- Clinical effects not seen for a few weeks
Lofepramine
TRICYCLIC ANTIDEPRESSANT
Actions: antidepressant
MOA: inhibits reuptake of NA and 5HT3 into neurons, increasing transmitter actions
Use: depression, panic disorder, neuropathic pain
Side effects: sedation, blurred vision, dry mouth, constipation, urinary retention
- Overdose potentially fatal due to cardiac dysrhythmia, severe hypotension, seizure and CNS depression
- Increased risk of suicide in younger patients
- Clinical effects not seen for a few weeks
Citalopram
SSRI - Selective serotonin reuptake inhibitor
Action: antidepressant
MOA: Inhibits the reuptake of 5HT3 into neurons
Use: depression, anxiety
Side effects: anxiety and insomnia. Nausea, diarrhoea, headache, sexual dysfunction
- Increased risk of suicide in younger patients
- Causes hyponatraemia in the elderly
Fluoxetine
SSRI - Selective serotonin reuptake inhibitor
Action: antidepressant
MOA: Inhibits the reuptake of 5HT3 into neurons
Use: depression, anxiety
Side effects: anxiety and insomnia. Nausea, diarrhoea, headache, sexual dysfunction
- Increased risk of suicide in younger patients
- Causes hyponatraemia in the elderly
Sertraline
SSRI - Selective serotonin reuptake inhibitor
Action: antidepressant
MOA: Inhibits the reuptake of 5HT3 into neurons
Use: depression, anxiety
Side effects: anxiety and insomnia. Nausea, diarrhoea, headache, sexual dysfunction
- Increased risk of suicide in younger patients
- Causes hyponatraemia in the elderly
Paroxetine
SSRI - Selective serotonin reuptake inhibitor
Action: antidepressant
MOA: Inhibits the reuptake of 5HT3 into neurons
Use: depression, anxiety
Side effects: anxiety and insomnia. Nausea, diarrhoea, headache, sexual dysfunction
- Increased risk of suicide in younger patients
- Causes hyponatraemia in the elderly
Duloxetine
SNRI - serotonin, NA reuptake inhibitor
Actions: antidepressant
MOA: inhibits the reuptake of 5HT and NA into neurons, increasing transmitter action
Use: depression, panic disorder, GAD, social phobia
Side effects: nausea, headache, sleep disturbance, sexual dysfunction
- cardiac dysrhythmia, seizure and CNS depression with OD
- takes a few weeks to see effects
- increase risk of suicide in younger people
Venlafaxine
SNRI - serotonin, NA reuptake inhibitor
Actions: antidepressant
MOA: inhibits the reuptake of 5HT and NA into neurons, increasing transmitter action
Use: depression, panic disorder, GAD, social phobia
Side effects: nausea, headache, sleep disturbance, sexual dysfunction
- cardiac dysrhythmia, seizure and CNS depression with OD
- takes a few weeks to see effects
- increase risk of suicide in younger people
Reboxetine
NRI - NA reuptake inhibitor
Actions: antidepressant
MOA: inhibits selectively the reuptake of NA.
Use: depression, panic disorder
Side effects: insomnia, headache
- Does not increase risk of suicide
Phenelzine
MOAIs - monamine oxidase inhibitor
Actions: antidepressant
MOA: Irreversibly binds to A and B forms of monoamine oxidase.
MAO-A acts on NA and 5HT
MAO-B acts on dopamine
Inhibiting MAO increases transmitter at nerve endings
Use: atypical depression. social phobia
Side effects: postural hypotension, headache, insomnia, sexual dysfunction
Dry mouth, urinary retention
- OD = convulsions
- Increased risk of suicide in young people
- Dietary TYRAMINE causes hypertensive crisis (Cheese)
- Antidepressant effect due to MAO-A inhibition
Moclobemine
MOAIs - monamine oxidase inhibitor (A only)
Actions: antidepressant
MOA: Irreversibly binds to A forms of monoamine oxidase.
MAO-A acts on NA and 5HT
Inhibiting MAO increases transmitter at nerve endings
Use: atypical depression. social phobia
Side effects: postural hypotension, headache, insomnia, sexual dysfunction
Dry mouth, urinary retention
- OD = convulsions
- Increased risk of suicide in young people
- Dietary TYRAMINE causes hypertensive crisis (Cheese)
- Antidepressant effect due to MAO-A inhibition
Isocarboazid
MOAIs - monamine oxidase inhibitor
Actions: antidepressant
MOA: Irreversibly binds to A and B forms of monoamine oxidase.
MAO-A acts on NA and 5HT
MAO-B acts on dopamine
Inhibiting MAO increases transmitter at nerve endings
Use: atypical depression. social phobia
Side effects: postural hypotension, headache, insomnia, sexual dysfunction
Dry mouth, urinary retention
- OD = convulsions
- Increased risk of suicide in young people
- Dietary TYRAMINE causes hypertensive crisis (Cheese)
- Antidepressant effect due to MAO-A inhibition
Mirtazipine
Alpha adrenoceptor and 5HT receptor antagonist
Actions: antidepressant
MOA: Antagonist at presynaptic alpha 2 adrenoceptors, preventing inhibitory effects of NA on 5HT
Use: major depression, PTSD
Side effects: increased appetite, weight gain
Agranulocytosis (rare)
Bupropion
DOPAMINE REUPTAKE INHIBITOR
Actions: atypical antidepressant, used in smoking cessation
MOA: inhibits neuronal dopamine reuptake with a lesser effect on NA
Antagonist at nictonic receptors
Use: alone or in combination with SSRIs in depression
Side effects: agitation, tremor, dry mouth, nausea, insomnia, skin rashes
Seizures can occur with large doses
Mesalazine
Aminosalicylate
Action: anti-inflammatory
MOA; Not well understood. ?blocking COX to reduce local inflammatory response
Use: UC. Crohn’s
SE: diarrhoea, nausea and vomiting, abdo pain, headache, hypersensitivity reactions.
Can cause blood disorders
NOTE: must monitor renal function before and during treatment
Prednisolone
Glucocorticoid
Action: anti-inflammatory. immunosuppressant
MOA: inhibits clonal proliferation of T and B cells and macrophage activation. Reduces chronic inflammation, autoimmune and hypersensitivity reactions
Inhibits transcription of genes for various cytokines including IL2
Use: IBD. prevent organ rejection
SE: decrease response to infection. osteoporosis, Cushings, suppresses endogenous GC
Budesonide
Glucocorticoid
Action: anti-inflammatory. immunosuppressant
MOA: inhibits clonal proliferation of T and B cells and macrophage activation. Reduces chronic inflammation, autoimmune and hypersensitivity reactions
Inhibits transcription of genes for various cytokines including IL2
Use: IBD. prevent organ rejection
SE: decrease response to infection. osteoporosis, Cushings, suppresses endogenous GC
Ciclosporin
Immunosuppressant
Action: decreases cell mediated immune response. Interferes with T cell differentiation and clonal proliferation of T cells
MOA: complexes with cyclophilin to inhibit calcineurin to prevent transcription of IL2
Use: organ rejection, graft vs. host, Crohn’s
SE: nephrotoxic, hypertension, hepatotoxic, GI disturbances, tremor, hirsuitism, paraesthesia, gum atrophy
Azathioprine
Antiproliferative immunosuppressant
Action: decreases clonal proliferation of T and B cells during induction phase of immune response
MOA: interferes with purine synthesis. cytotoxic on dividing cells
Use: UC and Crohn’s. prevent organ rejection. chronic autoimmune disease
SE: myelotoxicity. GI disturbance. hypersensitivity reactions
NOTE: monitor blood for myelosuppression
Mercaptopurine
Antiproliferative immunosuppressant/ antimetabolite cancer agent
Action: decreases clonal proliferation of T and B cells during induction phase of immune response
MOA: interferes with purine synthesis. cytotoxic on dividing cells
Use: UC and Crohn’s. prevent organ rejection. chronic autoimmune disease
SE: myelotoxicity. GI disturbance. hypersensitivity reactions
NOTE: monitor blood for myelosuppression
Infliximab
Cytokine inhibitor -
Action: decreased inflammation
MOA: monoclonal antibody against TNF alpha
Use: Crohns, UC, RA
SE; nausea and vomiting. headache. URTI. Blood dyscrasis
Note: half mouse, half human
Omeprazole
Proton pump inhibitor
Action: inhibition of gastric acid secretion
MOA: binds irreversibly to H+/K+ ATPase in gastric parietal cells and inhibits H+ transport
Use: gastro/duodenal ulcers, GORD, Zollinger Ellison syndrome, H.pylori, NSAID ulcers
SE: usually sage, headache, adbo pain, diarrhoea, flatulence, nausea
Lansoprazole
Proton pump inhibitor
Action: inhibition of gastric acid secretion
MOA: binds irreversibly to H+/K+ ATPase in gastric parietal cells and inhibits H+ transport
Use: gastro/duodenal ulcers, GORD, Zollinger Ellison syndrome, H.pylori, NSAID ulcers
SE: usually sage, headache, adbo pain, diarrhoea, flatulence, nausea
Ranitidine
H2 receptor antagonist
Action: inhibits gastric acid secretion. Inhibits action of histamine released from mast like cells in gastric mucosa
MOA: selective, reversible, competitive antagonism of H2 histamine receptors on parietal cells
Use: peptic and duodenal ulcers. GORD. NSAID ulcers
SE: uncommon. headache, GIT disturbance, dizziness
NOTE; many drug interactions
Cimetidine
H2 receptor antagonist
Action: inhibits gastric acid secretion. Inhibits action of histamine released from mast like cells in gastric mucosa
MOA: selective, reversible, competitive antagonism of H2 histamine receptors on parietal cells
Use: peptic and duodenal ulcers. GORD. NSAID ulcers
SE: uncommon. headache, GIT disturbance, dizziness
NOTE; many drug interactions
Terlipressin
ADH analogue
Action: vasoconstriction
MOA: analogue of vasopressin/ADH. Vasoconstricts blood vessels. Also acts to allow urine to be more concentrated
Use: splenic vasoconstriction in varices
SE: hyponatraemia, anaphylaxis, bronchospasm
Loperamide
ANTI-DIARRHOEAL
Actions: decreases gut motility and secretions. Slower transit allows increase fluid absorption
MOA: mu opioid receptor agonist in myenteric plexus to inhibit peristalsis. Few central effects (analgesia and addiction)
Use: acute or chronic diarrhoea
SE: drowsiness and nausea. Constipation and abdominal cramps. CNS depression in OD.
Note: effects reversed by naloxone.
4mg initially then 2mg after each stool for up to 5 days.
Investigations for chronic diarrhoea
Basic:
- FBC, LFTs, Calcium, B12, folate, iron, TFTs, coeliac screen
- If symptoms suggest functional disease and under 45, normal investigations = IBS
History of malabsorption
- Small bowel = endoscopy + biopsy
- Pancreatic: faecal elastase, chymotrypsin then ERCP or MRCP
History of colonic/terminal ileum disease
- Flexisig if under 45
- Colonoscopy if over 45
Difficult
- laxative use
- high volume
- normal investigations
- then consider inpatient with stool weights and laxative screen
Macrogol
OSMOTIC LAXATIVE
MOA: poorly absorbed and raises osmotic load within gut lumen. Causes ingested water to be retained, increasing fluid volume in gut promotes movement.
Use: bowel cleansing prior to examination. Constipation
SE: abdo cramps, few systemic actions due to poor absorption
Note: effects develop over 2-3 days
Lactulose
OSMOTIC LAXATIVE
MOA: poorly absorbed and raises osmotic load within gut lumen. Causes ingested water to be retained, increasing fluid volume in gut promotes movement.
Use: bowel cleansing prior to examination. Constipation
SE: abdo cramps, few systemic actions due to poor absorption
Note: effects develop over 2-3 days
Lubiprostone
CHLORIDE CHANNEL ACTIVATOR
Actions: increase fluid content of the gut, aiding propulsive movement
MOA: chloride channel activator of gut epithelium. Enhanced Cl- secretion is accompanied by water, increasing intraluminal fluid and movement through the bowel.
Use: chronic constipation. IBS with constipatiton.
SE: Nausea and diarrhoea.
Docusate
STOOL SOFTENER
Actions: softens and lubricates the stool to allow easier passage
MOA: surfactant with emulsifying action
Use: constipation and haemorrhoids
Methylcellulose
BULK FORMING LAXATIVE
Actions: laxative
MOA: poorly absorbed, hydroscopic, forms a soft faecal mass which descends through the gut to promote peristalsis
Use: constipation
SE: flatulence. few systemic actions. obstruction
Ispaghula husk
BULK FORMING LAXATIVE
Actions: laxative
MOA: poorly absorbed, hydroscopic, forms a soft faecal mass which descends through the gut to promote peristalsis
Use: constipation
SE: flatulence. few systemic actions. obstruction
Bisacodyl
STIMULANT LAXATIVE
MOA: active metabolite stimulates peristalsis by irritation of mucosa plus an effect on enteric nervous system. Increases fluid volume by increasing secretion.
Use: chronic constipation. bowel cleansing, prior to examination.
SE: abdominal cramps. Tolerance to action with atony of colon with excessive use
Senna
STIMULANT LAXATIVE
MOA: active metabolite stimulates peristalsis by irritation of mucosa plus an effect on enteric nervous system. Increases fluid volume by increasing secretion.
Use: chronic constipation. bowel cleansing, prior to examination.
SE: abdominal cramps. Tolerance to action with atony of colon with excessive use
Senna is activated by colonic bacteria
Hyoscine
MUSCARINIC RECEPTOR ANTAGONIST
Action: inhibits secretions. Tachycardia. Relaxes smooth muscle, inhibiting peristalsis. Antiemetic
MOA: competitive reversible antagonism at all muscarinic receptors
Use: IBS, motion sickness, urinary incontinence
SE: constipation, hyperthermia, dry mouth, urinary retention, blurred vision
Atropine
MUSCARINIC RECEPTOR ANTAGONIST
Action: inhibits secretions. Tachycardia. Relaxes smooth muscle, inhibiting peristalsis. Antiemetic
MOA: competitive reversible antagonism at all muscarinic receptors
Use: IBS, motion sickness, urinary incontinence
SE: constipation, hyperthermia, dry mouth, urinary retention, blurred vision
Metronidazole
Antibiotic
MOA: exact mechanism unclear. Causes bacterial damage to anaerobic organisms via nitro group.
Use: anaerobic infections (1st line for c.diff), sepsis, protozoal and dental infections. H pylori
SE: GI disturbance, metallic taste, dizziness, headache, pancreatitis, peripheral neuropathy
NOTE: INTERACTS WITH ALCOHOL
Avoid during and 48 hours after stopping
Interactions with warfarin
Ramipril
ACE inhibitor
Actions: decrease BP by decreasing vasoconstrictor tone and cardiac load
MOA: inhibits angiotensin converting enzyme, to decrease synthesis of angiotensin II. Decrease aldosterone secretion, Increase salt and water excretion. Decrease plasma volume and cardiac load
Use: hypertension. heart failure. ventricular dysfunction post-MI. Diabetic nephropathy
SE: Hypotension. Dry cough. Angioedema,. Renal failure
NOTE: hyperkalaemia if given with k+ sparing diuretics
Dry cough is due to production of bradykinin by stimulating kallikerin-kinin system
Losartan
ARB
Actions: Lowers BP by decreasing vasoconstrictor tone
MOA: Blocks action of angiotensin II
Use: hypertension. Congestive heart failure. Nephropathy
SE: hypotension, dizziness, hyperkalaemia
Lisinopril
ACE inhibitor
Actions: decrease BP by decreasing vasoconstrictor tone and cardiac load
MOA: inhibits angiotensin converting enzyme, to decrease synthesis of angiotensin II. Decrease aldosterone secretion, Increase salt and water excretion. Decrease plasma volume and cardiac load
Use: hypertension. heart failure. ventricular dysfunction post-MI. Diabetic nephropathy
SE: Hypotension. Dry cough. Angioedema,. Renal failure
NOTE: hyperkalaemia if given with k+ sparing diuretics
Dry cough is due to production of bradykinin by stimulating kallikerin-kinin system
Candesartan
ARB
Actions: Lowers BP by decreasing vasoconstrictor tone
MOA: Blocks action of angiotensin II
Use: hypertension. Congestive heart failure. Nephropathy
SE: hypotension, dizziness, hyperkalaemia
Glyceryl trinitrate
Actions: dilates and relaxes vascular smooth muscle and decreases cardiac work and metabolic demand while increasing perfusion and oxygenation of cardiac muscle
MOA: Gives rise to NO which activates PKG and reduces contraction. Dilates venous vessels to decrease preload. Dilates arterial vessels to decrease afterload.
ADE: sublingual, acts immediately and lasts for 30 minutes
Use: prevent or treat stable angina. IV in unstable angina
SE: headache, postural hypotension, tolerance with prolonged use.
Isosorbide dinitrate
Actions: dilates and relaxes vascular smooth muscle and decreases cardiac work and metabolic demand while increasing perfusion and oxygenation of cardiac muscle
MOA: Gives rise to NO which activates PKG and reduces contraction. Dilates venous vessels to decrease preload. Dilates arterial vessels to decrease afterload.
ADE: sublingual, acts immediately and lasts for 30 minutes
Use: prevent or treat stable angina. IV in unstable angina
SE: headache, postural hypotension, tolerance with prolonged use.
Furosemide
LOOP DIURETIC
Actions: causes copious urine production by inhibiting NaCl reabsorption in thick ascending loop. Increases excretion of calcium and magnesium
MOA: Inhibits Na/K/2Cl co-transporter in the luminal membrane by combining with chloride binding site
Use: pulmonary oedema, chronic heart failure, ascites, hypercalcaemia, hyperkalaemia
SE: hypokalaemic acidosis, hyperuricaemia (can precipitate gout), hypovolaemia, hypotension in elderly, reversible ototoxicity
Bumetanide
LOOP DIURETIC
Actions: causes copious urine production by inhibiting NaCl reabsorption in thick ascending loop. Increases excretion of calcium and magnesium
MOA: Inhibits Na/K/2Cl co-transporter in the luminal membrane by combining with chloride binding site
Use: pulmonary oedema, chronic heart failure, ascites, hypercalcaemia, hyperkalaemia
SE: hypokalaemic acidosis, hyperuricaemia (can precipitate gout), hypovolaemia, hypotension in elderly, reversible ototoxicity
Bendroflumethiazide
THIAZIDE DIURETIC
Actions: causes moderate degree of diuresis by inhibiting NaCl reabsorption in the distal tubule. Increase potassium and H+ excretion.
MOA: inhibits the Na/Cl co-transporter in the luminal membrane of the distal convoluted tubule
Use: hypertension. mild heart failure. nephrogenic diabetes insipidus. kidney stones
SE: potassium loss. metabolic alkalosis, hyperuricaemia (can precipitate gout), increased insulin requirement, erectile dysfunction
Metolazone
THIAZIDE DIURETIC
Actions: causes moderate degree of diuresis by inhibiting NaCl reabsorption in the distal tubule. Increase potassium and H+ excretion.
MOA: inhibits the Na/Cl co-transporter in the luminal membrane of the distal convoluted tubule
Use: hypertension. mild heart failure. nephrogenic diabetes insipidus. kidney stones
SE: potassium loss. metabolic alkalosis, hyperuricaemia (can precipitate gout), increased insulin requirement, erectile dysfunction
Spironolactone
K+ sparing diuretic
Actions: inhibits Na+ reabsorption in distal nephron. limited diuretic efficacy. decreased potassium excretion
MOA: competitive antagonist of aldosterone. Causes diuresis by preventing production of aldosterone mediator that normally causes Na influx
Use: hypertension. Primary and secondary hyperaldosteronism
SE: Hyperkalaemia. Hyperchloraemic acidosis. Gynaecomastia
Eplerenone
K+ sparing diuretic
Actions: inhibits Na+ reabsorption in distal nephron. limited diuretic efficacy. decreased potassium excretion
MOA: competitive antagonist of aldosterone. Causes diuresis by preventing production of aldosterone mediator that normally causes Na influx
Use: hypertension. Primary and secondary hyperaldosteronism
SE: Hyperkalaemia. Hyperchloraemic acidosis. Gynaecomastia
Bisoprolol
BETA BLOCKER
Actions: antidysrhythmic. antihypertensive. antianginal. blocks action of catecholamines on beta adrenoceptors
MOA: blocks sympathetic drive and decreases pacemaker activity by increasing AV conduction time.
BETA 1 SELECTIVE
Use; hypertension. decreased mortality after infarct. paroxysmal AF
SE: bronchoconstriction in asthmatics
Cardiac slowing with possible heart block
Carvedilol
BETA BLOCKER
Actions: antidysrhythmic. antihypertensive. antianginal. blocks action of catecholamines on beta adrenoceptors
MOA: blocks sympathetic drive and decreases pacemaker activity by increasing AV conduction time.
BETA 1 SELECTIVE
Use; hypertension. decreased mortality after infarct. paroxysmal AF
SE: bronchoconstriction in asthmatics
Cardiac slowing with possible heart block
Amiloride
K+ sparing diuretic
Actions: inhibits Na+ reabsorption in distal nephron. limited diuretic efficacy. decreased potassium excretion
MOA: competitive antagonist of aldosterone. Causes diuresis by preventing production of aldosterone mediator that normally causes Na influx
Use: hypertension. Primary and secondary hyperaldosteronism
SE: Hyperkalaemia. Hyperchloraemic acidosis. Gynaecomastia
Indapamide
THIAZIDE LIKE DIURETIC
Actions: causes moderate degree of diuresis by inhibiting NaCl reabsorption in the distal tubule. Increase potassium and H+ excretion.
MOA: inhibits the Na/Cl co-transporter in the luminal membrane of the distal convoluted tubule
Use: hypertension. mild heart failure. nephrogenic diabetes insipidus. kidney stones
SE: potassium loss. metabolic alkalosis, hyperuricaemia (can precipitate gout), increased insulin requirement, erectile dysfunction
Amlodipine
Calcium channel blocker dihydropyridine
Action: vascular dilation, decrease BP.. Dilate arterial resistance vessels.
MOA; Blocks voltage gated calcium channels in vascular smooth muscle, inhibiting calcium influx and contraction
Use: hypertension. angina
Side effects: reflex tachycardia. hypotension. headache
Nifedipine
Calcium channel blocker dihydropyridine
Action: vascular dilation, decrease BP.. Dilate arterial resistance vessels.
MOA; Blocks voltage gated calcium channels in vascular smooth muscle, inhibiting calcium influx and contraction
Use: hypertension. angina
Side effects: reflex tachycardia. hypotension. headache
Verapamil
Calcium channel blocker NON-dihydropyridine
Action: vascular dilation, decrease BP.. Dilate arterial resistance vessels.
MOA; Blocks voltage gated calcium channels in vascular smooth muscle, inhibiting calcium influx and contraction
Use: hypertension. angina
Side effects: reflex tachycardia. hypotension. headache
Atenolol
Beta blocker (Beta 1)
Action: decrease BP by decreasing cardiac output, decreased renin release, decreased sympathetic activity
MOA: Blocks action of endogenous and exogenous agonists on beta 1 receptors
Use: Hypertension. Angina. Prevent of dysrhythmia in MI
SE: Bronchoconstriction in asthma. Potential heart block/failure in coronary disease. Decreased warning in hypoglycaemia. Cold extremities. Fatigue.
Beta 1 selective
Propranolol
Beta blocker
Action: decrease BP by decreasing cardiac output, decreased renin release, decreased sympathetic activity
MOA: Blocks action of endogenous and exogenous agonists on beta 1 receptors
Use: Hypertension. Angina. Prevent of dysrhythmia in MI
SE: Bronchoconstriction in asthma. Potential heart block/failure in coronary disease. Decreased warning in hypoglycaemia. Cold extremities. Fatigue.
Metoprolol
Beta blocker (Beta 1)
Action: decrease BP by decreasing cardiac output, decreased renin release, decreased sympathetic activity
MOA: Blocks action of endogenous and exogenous agonists on beta 1 receptors
Use: Hypertension. Angina. Prevent of dysrhythmia in MI
SE: Bronchoconstriction in asthma. Potential heart block/failure in coronary disease. Decreased warning in hypoglycaemia. Cold extremities. Fatigue.
Beta 1 selective
Doxazosin
Alpha 1 receptor antagonist
Actions: vasodilation and decreased BP. Increased HR in response to hypotension. Decreased bladder sphincter tone. Inhibition of hypertrophy of smooth muscle of bladder neck and prostate capsule.
MOA: block action of endogenout and exogenous agonists on alpha receptros
Use: severe hypertension. BPH
SE: orthostatic hypotension, dizziness, hypersensitivity reaction, insomnia, priapism, abnormal ejaculation
Tamsulosin
Alpha 1 receptor antagonist
Actions: vasodilation and decreased BP. Increased HR in response to hypotension. Decreased bladder sphincter tone. Inhibition of hypertrophy of smooth muscle of bladder neck and prostate capsule.
MOA: block action of endogenous and exogenous agonists on alpha receptors
Use: severe hypertension. BPH
SE: orthostatic hypotension, dizziness, hypersensitivity reaction, insomnia, priapism, abnormal ejaculation
Diltiazem
Calcium channel blocker NON-dihydropyridine
Action: vascular dilation, decrease BP.. Dilate arterial resistance vessels.
MOA; Blocks voltage gated calcium channels in vascular smooth muscle, inhibiting calcium influx and contraction
Use: hypertension. angina
Side effects: reflex tachycardia. hypotension. headache
Bendroflumethazide
THIAZIDE DIURETIC
Actions: moderate degree of diuresis by inhibiting NaCl reabsorption in distal tubule. increased potassium and H+ excretion. Decreased excretion of calcium and uric acid
MOA: inhibits Na/Cl- co-transporter in luminal membrane of distal tubule
Use: hypertension. mild heart failure. nephrogenic diabetes insipidus. kidney stones
SE: hypokalaemia. metabolic alkalosis. hyperuricaemia (gout), increased insulin requirement, erectile dysfunction
Simvastatin
HMG-CoA reductase inhibitor
Actions: decrease LDL. Some decrease of plasma triglyceride and some raise in HDL
MOA: specific reversible competitive inhibition of rate limiting enzyme HMG CoA reductase and thus decreased hepatic cholesterol synthesis which upregulates LDL
Use: hypercholesterolaemia. prevent raised cholesterol. infarction
SE: muscle pain. GIT disturbance. insomnia. rash.
Severe: myositis (rare)
Atorvastatin
HMG-CoA reductase inhibitor
Actions: decrease LDL. Some decrease of plasma triglyceride and some raise in HDL
MOA: specific reversible competitive inhibition of rate limiting enzyme HMG CoA reductase and thus decreased hepatic cholesterol synthesis which upregulates LDL
Use: hypercholesterolaemia. prevent raised cholesterol. infarction
SE: muscle pain. GIT disturbance. insomnia. rash.
Severe: myositis (rare)
Gemfibrozil
Actions: marked decrease in plasma VLDL and triglyceride. Modest decrease in LDL and small increase in HDL
MOA: increase transcription for genes for lipoprotein lipase and apoproteins apoA1 and apoA5. Increased LDL uptake by receptors.
Use: mixed dyslipidaemia.
SE: GI upset. Rash. Moderate increase in gallstones. myositis
Do not give with a statin
Bezafibrate
Actions: marked decrease in plasma VLDL and triglyceride. Modest decrease in LDL and small increase in HDL
MOA: increase transcription for genes for lipoprotein lipase and apoproteins apoA1 and apoA5. Increased LDL uptake by receptors.
Use: mixed dyslipidaemia.
SE: GI upset. Rash. Moderate increase in gallstones. myositis
Do not give with a statin
Fenofibrate
Actions: marked decrease in plasma VLDL and triglyceride. Modest decrease in LDL and small increase in HDL
MOA: increase transcription for genes for lipoprotein lipase and apoproteins apoA1 and apoA5. Increased LDL uptake by receptors.
Use: mixed dyslipidaemia.
SE: GI upset. Rash. Moderate increase in gallstones. myositis
Do not give with a statin
Ezetimibe
Actions: inhibits absorption of cholesterol from intestine. Decreases LDL
MOA: Blocks sterol carrier protein in brush border of enterocytes. Decrease biliary and dietary cholesterol delivered to liver
Use: hypercholesterolaemia, usually adjunct to statin
SE: few. GI upsets. Headaches. Rashes. Myalgia
Aspirin
Non-steroidal drug with antithrombotic and anti-inflammatory properties
Actions: antiplatelet. analgesic. anti-inflammatory
MOA: irreversibly inactivates COX1. Alters balance between TXA2 and PGI2 in platelets and vascular endothelium
Use: decrease risk of MI or TIA. Stroke.
SE: GI bleeding. Bronchospasm. Toxic doses cause respiratory alkalosis followed by acidosis
LMWH
Action: Anticoagulant
MOA: accelerates action of antithrombin III by increasing its inactivation of factor Xa
Use: VTE prevention. Treat DVT, PE, MI and unstable angina
ADE: given subcut, renally excreted
SE: bleeding. less likely than heparin to cause thrombocytopaenia. Hypersensitivity reactions. osteoporosis
- Blood tests prior to starting: APTT, PT, U&Es, platelets
- No routine monitoring
- Takes up to 5 days to reach therapeutic range
Dalteparin
Action: Anticoagulant
MOA: accelerates action of antithrombin III by increasing its inactivation of factor Xa
Use: VTE prevention. Treat DVT, PE, MI and unstable angina
Dose calculated via body weight
ADE: given subcut, renally excreted
SE: bleeding. less likely than heparin to cause thrombocytopaenia. Hypersensitivity reactions. osteoporosis
- Blood tests prior to starting: APTT, PT, U&Es, platelets
- No routine monitoring
- Takes up to 5 days to reach therapeutic range
Fondaparinux
Action: Anticoagulant
MOA: accelerates action of antithrombin III by increasing its inactivation of factor Xa
Use: VTE prevention. Treat DVT, PE, MI and unstable angina
ADE: given subcut, renally excreted
SE: bleeding. less likely than heparin to cause thrombocytopaenia. Hypersensitivity reactions. osteoporosis
- Blood tests prior to starting: APTT, PT, U&Es, platelets
- No routine monitoring
- Takes up to 5 days to reach therapeutic range
Heparin
Action: inhibits blood coagulation
MOA: accelerates action of antithrombin III increasing its activation mainly of factors 1a and 10a
Use: Treat DVT, PE, UA and peripheral arterial occlusion
SE: Bleeding, thrombocytopaenia, hypersensitivity reaction, osteoporosis
Warfarin
Action: inhibits blood coagulation
MOA; inhibits reduction of vitamin K and prevents gamma-carboxylation of glutamate residue in factors 2, 7, 9 and 10
ADE: oral, slow onset
Use: treat DVT, PE and prevent embolism in AF
Side effects: Bleeding ++ drug interactions
Note
- Regular INR checks
- Lots of drug interactions due to cytochrome p450
- Regular diet avoiding vitamin K rich foods
Rivaroxaban
Action: inhibits blood coagulation
MOA: Direct inhibitor of Xa
Use: treat DVT and PE. Prevention of VTE
Note: requires no monitoring, beneficial over warfarin
NOT reversible
More expensive
Dabigatran
Action: inhibits blood coagulation
MOA: Direct inhibitor of Xa
Use: treat DVT and PE. Prevention of VTE
Note: requires no monitoring, beneficial over warfarin
More expensive, but decreased monitoring costs
Reversible - idarucizumab
methotrexate
DMARD/ ANTIMETABOLITE (cancer)
Actions: marked anti-inflammatory action. Cytotoxic in large doses
MOA: Folate antagonist and therefore interferes with thymidylate synthesis (essential for DNA synthesis)
Use: RA, psoriasis, ankylosing spondylitis, polymyositis, cancer
Side effects: GI disturbance, dose related liver toxicity, bone marrow suppression, pneumonitis
Contraindications: pregnancy, breast feeding, immunodeficiency syndromes, impaired renal or liver function
Chlorpromazine
Typical antipsychotic
Actions: antipsychotic. apathy and inertia. decreased aggression. antiemetics.
MOA: competitive antagonism of dopamine D2 receptors in mesolimbic and cortical pathways.
Use: Schizophrenia. Psychosis. manic phase of bipolar. Tourette’s. Nausea and vomiting. Aggression in children.
Side effects: Marked sedation Extrapyramidal symptoms Galactorrhoea.; Gynaemcomastia. Weight gain. Contipation. Dry mouth. Hypotension
Rare: neuroleptic malignant syndrome
Agranulocytosis. hepatotoxicity
Haloperidol
Typical antipsychotic
Actions: antipsychotic. apathy. decreased aggression. antiemetic
MOA: competitive antagonism of dopamine D2 receptors. Increased potency when compared with chlorpromazine
Use: Schizophrenia. Psychosis. Mania. Aggressive behaviour. Tourette’s
Side effects: Marked EPS Hyperprolactinaemia Sedative. Hypotensive Neuroleptic malignant syndrome
Flupentixol
Typical antipsychotic
Action: antipsychotic. antidepressant
MOA: competitive antagonism of dopamine D2 receptors.
Use: schizophrenia. psychosis. bipolar disorders.
Side effects: EPS, hyperprolactinaemia, neuroleptic malignant syndrome
Clozapine
Atypical antipsychotic
Action: antipsychotic. effective against positive and negative symptoms
MOA: Actions of 5HT2, muscarinic, alpha 1 adrenoceptors, H1 receptors antagonists.
Use: schizophrenia. Very effective, often used in resistant patients.
Side effects:
Little EPS, constipation, agranulocytosis, epileptic seizures, weight gain, hyperglycaemia, hypotension
Rare: neutropaenia, thromboembolism, cardiomyopathy, myocarditis, aspiration pneumonia
Olanzipine
Atypical antipsychotic
Action: antipsychotic. effective against positive and negative symptoms
MOA: Actions of 5HT2, muscarinic, alpha 1 adrenoceptors, H1 receptors antagonists.
Use: schizophrenia. Very effective, often used in resistant patients.
Side effects:
Little EPS, constipation, agranulocytosis, epileptic seizures, weight gain, hyperglycaemia, hypotension
Risperidone
Atypical antipsychotic
Actions: antipsychotic. effective against positive and negative symptoms
MOA: Potent antagonists of D2 and 5HT2 and alpha 1 adrenoceptors.
Use: Schizophrenia. Psychosis. Mania.
Side effects: EPS (more than other atypicals), insomnia, sedation, hyperprolactinaemia, weight gain, hypotension, sexual dysfunction, anxiety
Quetiapine
Atypical antipsychotic
Actions: antipsychotic.
MOA: antagonism of D2 and 5HT2 receptors.
Use: schizophrenia and other psychotic states. Bipolar disorder.
Side effects: Weight gain. Hyperprolactinaemia Minor EPS. Constipation. Dry mouth. Sedation. postural hypotension. Rare: neuroleptic malignant syndrome
Sulpiride
Atypical antipsychotic
Actions: antipsychotic.
MOA: Dopamine D2 and D3 antagonism. preferential action on dopamine autoreceptors - less EPS.
Use: schizophrenia
Side effects: hyperprolactinaemia. insomnia. anxiety. weight gain. constipation. dry mouth
Amisulpiride
Atypical antipsychotic
Actions: antipsychotic.
MOA: Dopamine D2 and D3 antagonism. preferential action on dopamine autoreceptors - less EPS.
Use: schizophrenia
Side effects: hyperprolactinaemia. insomnia. anxiety. weight gain. constipation. dry mouth
Aripiprazole
Actions: antipsychotic
MOA: Modifications of dopaminergic transmission. Strongly D2 with partial agonist activity.
Use: schizophrenia. psychosis. manic phase of bipolar
Side effects: fewer side effects than other antipsychotics.
Less weight gain.
Some hypotension and nausea and vomiting.
Lithium
Actions: mood stabiliser
MOA: not well established. Theory that lithium interferes with membrane ion transport including neurotransmitter uptake
Use: bipolar. mania. effects develop over 3-4 weeks
Side effects:
- Diarrhoea, tremor, confusion.
- Renal toxicity
- Decreases thyroid function
- Many drug interactions (particularly diuretics)
- In OD = convulsions, coma and death
Carbamazepine
Action: antiepileptic. Relieves neuropathic pain. Mood stabiliser
MOA: Blocks Na+ channels to inhibit action potential initiation and propagation. use-dependence of block means that action is preferential on rapid fire neurons
Use: partial and generalised seizures. Not absence seizures. Neuropathic pain. Bipolar disorder
Side effects: drowsiness, headache, mental disorientation, motor disturbances
Rare but serious: agranulocytosis, liver damage, aplastic anaemia
Teratogenic
p450 interaction
Sodium valproate
Actions: anticonvulsant, mood stabiliser
MOA: block of Na channels in inhibit action potential initiation and propagation. Inhibition of GABA transaminase to decrease GABA breakdown
Use: epilepsy. manic phase of bipolar, migraine
Side effects: nausea and vomiting. tremor. weight gain. reproductive dysfunction. hepatic and pancreatic toxicity
Teratogenic
Insulin
Increases tissue uptake and storage of glucose, fats and amino acids. Decreases blood glucose. Inhibits glycogenolysis and gluconeogenesis. Increases glycogen synthesis; Inhibits lipolysis
MOA: binds to its receptor and causes autophosphorylation of receptor.
Use: type 1 and type 2 DM. Emergency treatment of DKA
Side effects: hypoglycaemia. weight gain.
Metformin
BIGUANIDE
Actions: Lowers blood glucose
MOA: inhibits gluconeogenesis in liver by activating AMP-activated protein kinase. Increases glucose uptake into tissues
ADE: excreted unchanged in urine. Avoid in renal insufficiency
Use: T2DM, especially if obese
Side effects: GI upset, diarrhoea, anorexia.
Rare: lactic acidosis
DO NOT CAUSE HYPOGLYCAEMIA
Gliclazide
SULPHONYLUREA
Actions: Increased insulin release from functioning beta cells, producing insulin effects
MOA: Interaction with sulphonylurea receptor - subunit of K-ATP chanel in cell membrane of beta cells and causes K+ channels to close.
cell depolarises and activates calcium channels. Calcium channel opening stimulates exocytosis of insulin.
Use: T2DM
Side effects: hypoglycaemia. weight gain
Glimepiride
SULPHONYLUREA
Actions: Increased insulin release from functioning beta cells, producing insulin effects
MOA: Interaction with sulphonylurea receptor - subunit of K-ATP chanel in cell membrane of beta cells and causes K+ channels to close.
cell depolarises and activates calcium channels. Calcium channel opening stimulates exocytosis of insulin.
Use: T2DM
Side effects: hypoglycaemia. weight gain
Repaglinide
Metaglinide
Actions: decreased blood glucose concentration. Stimulates insulin release from beta cells
MOA: As sulphonylureas - interaction with K-ATP channel in cell membrane of beta cells and causes K+ channels to close.
Cell depolarises and activates calcium channels which stimulates exocytosis of insulin.
Use: T2DM
Side effects: hypoglycaemia
Pioglitazone
THIAZOLIDINEDIONE
Actions: decrease blood glucose concentration
MOA: activates PPAR-gamma in liver,fat and muscle to increase transcription of genes for proteins important in insulin action. Decrease glucose release from liver, increase muscle uptake and increased sensitivity to insulin.
Use: T2DM
Side effects: weight gain, fluid retention, hepatotoxic, Low risk of hypoglycaemia
Acarbose
GLUCOSIDASE INHIBITOR
Actions: delays carbohydrate absorption from intestine
MOA: Inhibits intestinal alpha-glucosidase and pancreatic amylase so decreases rise in blood glucose post-meal. It is responsible for breakdown of carbohydrates
Use: T2DM not controlled by other drugs
Side effects: GIT disturbance - flatulence, diarrhoea
Sitagliptin
DPP4 inhibitor
Actions: antidiabetic. Lowers blood sugar
MOA: competitive inhibition of DIPEPTIDYL PEPTIDASE 4 that breaks down GLP-1 hormones released in response to a meal. Stopping GLP1 deactivation, increased insulin secretion and decreased glucagon
Use: T2DM
Side effects: rare. nausea, headache, hypersensitivity reaction
Linagliptin
DPP4 inhibitor
Actions: antidiabetic. Lowers blood sugar
MOA: competitive inhibition of DIPEPTIDYL PEPTIDASE 4 that breaks down GLP-1 hormones released in response to a meal. Stopping GLP1 deactivation, increased insulin secretion and decreased glucagon
Use: T2DM
Side effects: rare. nausea, headache, hypersensitivity reaction
Canagliflozin
SGLT2 inhibitor
Action: decreased blood glucose. Decreases BP via osmotic diuresis
MOA: inhibitor of subtype 2 sodium glucose transport proteins (SGLT2) which are responsible for renal glucose absorption. Glucose is eliminated in urine
Use: T2DM
Side effects: increased UTI and genital infections. Decreased BP. Increased urination. Increased LDL and may increase risk of DKA
Dapagliflozin
SGLT2 inhibitor
Action: decreased blood glucose. Decreases BP via osmotic diuresis
MOA: inhibitor of subtype 2 sodium glucose transport proteins (SGLT2) which are responsible for renal glucose absorption. Glucose is eliminated in urine
Use: T2DM
Side effects: increased UTI and genital infections. Decreased BP. Increased urination. Increased LDL and may increase risk of DKA
Exenatide
GLP1 analogue
Actions: stimulates insulin secretion to decrease blood glucose
MOA: GLP1 agonist. GLP1 is released after a meal to stimulate insulin release. Slows gastric emptying. Decreased glucagon
Use: T2DM
Side effects: GIT disturbance. Dizziness or headache
Liraglitide
GLP1 analogue
Actions: stimulates insulin secretion to decrease blood glucose
MOA: GLP1 agonist. GLP1 is released after a meal to stimulate insulin release. Slows gastric emptying. Decreased glucagon
Use: T2DM
Side effects: GIT disturbance. Dizziness or headache
Empagliflozin
SGLT2 inhibitor
Action: decreased blood glucose. Decreases BP via osmotic diuresis
MOA: inhibitor of subtype 2 sodium glucose transport proteins (SGLT2) which are responsible for renal glucose absorption. Glucose is eliminated in urine
Use: T2DM
Side effects: increased UTI and genital infections. Decreased BP. Increased urination. Increased LDL and may increase risk of DKA
Saxagliptin
DPP4 inhibitor
Actions: antidiabetic. Lowers blood sugar
MOA: competitive inhibition of DIPEPTIDYL PEPTIDASE 4 that breaks down GLP-1 hormones released in response to a meal. Stopping GLP1 deactivation, increased insulin secretion and decreased glucagon
Use: T2DM
Side effects: rare. nausea, headache, hypersensitivity reaction
Bupropion
Dopamine reuptake inhibitor
Action: atypical antidepressant. elevated mood
MOA: relatively selective inhibitor of neuronal dopamine reuptake. Also antagonist at NICOTINIC receptors
Use: depression, smoking cessation
SE: Agitation, dry mouth, tremor, nausea, insomnia
Vareniciline
Start 1-2 weeks before stopping
Action: decreases cravings, decrease pleasure from tobacco
MOA: nicotinic receptor partial agonist
Less effect on dopamine than nicotine
SE: mild nausea, headaches, difficulty sleeping, nightmares
Use: smoking cessation
Nicotine replacement therapy
Patches, gum, nasal spray, mouth spray, inhalation, lozenge, sublingual tablet
Most effective the behavioural interventions
Contraindicated in CV disease or recent stroke
SE: Nausea, dizziness, flu like symptoms, palpitations, dyspepsia
Suxamethonium
Nicotinic receptor agonist
Depolarising neuromuscular blocker
Actions: short acting paralysis of skeletal muscle
MOA: Action on nicotinic receptors produces a maintained depolarisation of the muscle membrane. This inactivates Na+ channels which propagates action potential throughout the muscle.
Actions fail to spread along the fibres preventing muscle contraction in response to motor nerve activity.
ADE: Hydrolysed by cholinesterase within a few minutes. Small number of people have a lower activity enzyme
Use: short acting paralysis used in RSI and for short operative procedures
Not reversed by anticholinesterases
SE: hyperkalaemia. hypotension. bradycardia. muscle pain. raised intraocular pressure. malignant hyperthermia.
Succinylcholine
Also known as suxamethonium
Nicotinic receptor agonist
Depolarising neuromuscular blocker
Actions: short acting paralysis of skeletal muscle
MOA: Action on nicotinic receptors produces a maintained depolarisation of the muscle membrane. This inactivates Na+ channels which propagates action potential throughout the muscle.
Actions fail to spread along the fibres preventing muscle contraction in response to motor nerve activity.
ADE: Hydrolysed by cholinesterase within a few minutes. Small number of people have a lower activity enzyme
Use: short acting paralysis used in RSI and for short operative procedures
Not reversed by anticholinesterases
SE: hyperkalaemia. hypotension. bradycardia. muscle pain. raised intraocular pressure. malignant hyperthermia.
Pancuronium
Nicotinic receptor antagonist
Non-depolarising neuromuscular block
Actions: paralysis of skeletal muscle
MOA: reversible competitive antagonism at muscle type nicotinic receptors. Inhibits binding of ACh to the receptors at the muscle end-plate.
Fails to reach threshold for initiation and propagation. Action reversed by anticholinesterases.
ADE: substantial renal excretion
Use: general anaesthesia - aids intubation, muscle relaxation for surgery and aids mechanical ventilation
SE: tachycardia
Vecuronium
Nicotinic receptor antagonist
Non-depolarising neuromuscular block
Actions: paralysis of skeletal muscle
MOA: reversible competitive antagonism at muscle type nicotinic receptors. Inhibits binding of ACh to the receptors at the muscle end-plate.
Fails to reach threshold for initiation and propagation. Action reversed by anticholinesterases.
ADE: substantial renal excretion
Use: general anaesthesia - aids intubation, muscle relaxation for surgery and aids mechanical ventilation
SE: tachycardia
Rocuronium
Nicotinic receptor antagonist
Non-depolarising neuromuscular block
Actions: paralysis of skeletal muscle
MOA: reversible competitive antagonism at muscle type nicotinic receptors. Inhibits binding of ACh to the receptors at the muscle end-plate.
Fails to reach threshold for initiation and propagation. Action reversed by anticholinesterases.
ADE: substantial renal excretion
Use: general anaesthesia - aids intubation, muscle relaxation for surgery and aids mechanical ventilation
SE: tachycardia
Atracurium
Nicotinic receptor antagonist
Non-depolarising neuromuscular blocker
Actions: paralysis of skeletal muscle
MOA: reversible competitive antagonism at muscle type nicotinic receptors. Inhibits binding of ACh to receptors at muscle end-plate. Fails to reach threshold for initiation and propagation.
Use: general anaesthesia - aids tracheal intubation, muscle relaxation for general surgery, aids mechanical ventilation
SE: minor effects attributed to histamine release
Cisatricurium
Nicotinic receptor antagonist
Non-depolarising neuromuscular blocker
Actions: paralysis of skeletal muscle
MOA: reversible competitive antagonism at muscle type nicotinic receptors. Inhibits binding of ACh to receptors at muscle end-plate. Fails to reach threshold for initiation and propagation.
Use: general anaesthesia - aids tracheal intubation, muscle relaxation for general surgery, aids mechanical ventilation
SE: minor effects attributed to histamine release
Mivacurium
Nicotinic receptor antagonist
Non-depolarising neuromuscular blocker
Actions: paralysis of skeletal muscle
MOA: reversible competitive antagonism at muscle type nicotinic receptors. Inhibits binding of ACh to receptors at muscle end-plate. Fails to reach threshold for initiation and propagation.
Use: general anaesthesia - aids tracheal intubation, muscle relaxation for general surgery, aids mechanical ventilation
SE: minor effects attributed to histamine release
Neostigmine
Anticholinesterase
Actions: parasympathomimetic: increased peristalsis, increased secretions, bradycardia, bronchoconstriction, decreased intraocular pressure
MOA: reversible inhibition of acetylcholinesterase reduces breakdown of ACh at cholinergic nerve endings so potentiating transmitter action
Use: myasthenia gravis. reversal of non-depolarising neuromuscular block. Post-op urinary retention.
SE: may exacerbate asthma. Unwanted parasympathetic actions can be reduced by atropine.
Pyridostigmine
Anticholinesterase
Actions: parasympathomimetic: increased peristalsis, increased secretions, bradycardia, bronchoconstriction, decreased intraocular pressure
MOA: reversible inhibition of acetylcholinesterase reduces breakdown of ACh at cholinergic nerve endings so potentiating transmitter action
Use: myasthenia gravis. reversal of non-depolarising neuromuscular block. Post-op urinary retention.
SE: may exacerbate asthma. Unwanted parasympathetic actions can be reduced by atropine.
Edrophonium
Anticholinesterase
Actions: at neuromuscular junction - fasciculation and increased twitch tesions. parasympathetic actions: increased peristalsis, increased secretions, bradycardia, bronchoconstriction
MOA: Reversible inhibition of acetylcholinesterase reduces the breakdown of ACh at cholinergic nerve nedings so potentiating neurotransmission .
Only binds to anionic site - binding is reversed readily.
Use: diagnosis of myasthenia gravis. Action to short for therapeutic use.
Side effects: may exacerbate asthma. unwanted parasympathetic actions can be reduced with atropine.
Salbutamol
BETA 2 agonist
Actions: bronchodilation. Relaxes uterine smooth muscle.
MOA: decreased calcium mediated contraction in bronchioles. Increased cAMP which activates PKA. PKA inhibits myosin light chain kinase - mediator of contraction
Use: asthma. Acute attacks. COPD
Side effects: tremors, tachycardia, dysrhythmias, peripheral dilation.
Note: hypertensive crisis if used with MAO inhibitor.
Terbutaline
BETA 2 agonist
Actions: bronchodilation. Relaxes uterine smooth muscle.
MOA: decreased calcium mediated contraction in bronchioles. Increased cAMP which activates PKA. PKA inhibits myosin light chain kinase - mediator of contraction
Use: asthma. Acute attacks. COPD
Side effects: tremors, tachycardia, dysrhythmias, peripheral dilation.
Note: hypertensive crisis if used with MAO inhibitor.
Salmetrol
BETA 2 agonist
Actions: bronchodilation. Relaxes uterine smooth muscle.
MOA: decreased calcium mediated contraction in bronchioles. Increased cAMP which activates PKA. PKA inhibits myosin light chain kinase - mediator of contraction
Use: asthma. Nocturnal asthma, Exercised induced asthma. Long term therapy. COPD
Side effects: tremors, tachycardia, dysrhythmias, peripheral dilation.
Note: hypertensive crisis if used with MAO inhibitor.
Ibuprofen
NSAID
Actions: reduces inflammation, analgesic for inflammatory pain, antipyretic
MOA: reversible inhibition of COX1, weak inhibition of COX2
Use: inflammatory conditions. dysmenorrhoea
SE: GI disturbances. Gastric bleeding. headache, dizziness
NOTE: increased side effects if combined when combining NSAIDs. Used to close patent ductus arteriosus.
Naproxen
NSAID
Actions: reduces inflammation, analgesic for inflammatory pain, antipyretic
MOA: reversible inhibition of COX1, weak inhibition of COX2
Use: inflammatory conditions. dysmenorrhoea
SE: GI disturbances. Gastric bleeding. headache, dizziness
NOTE: increased side effects if combined when combining NSAIDs. Used to close patent ductus arteriosus.
More potent than ibuprofen.
Paracetamol
NSAID
Actions: analgesic. antipyretic. little inflammatory action.
MOA: Inhibition of COX 1 and COX2, also recently identified COX 3
Use: mild-moderate pain, especially headache. Most commonly used NSAID
SE: few and uncommon.
Toxic doses can cause nausea and vomiting and fatal liver toxicity.
Allopurinol
Uricosuric agent
Actions: reduces uric acid in the body
MOA: inhibits xanthine oxidase and the transformations of purines to xanthine.
Use: gout prevention
SE: Gi disturbance. Rashes and blood dyscrasias.
Note - not for acute gout. interferes with metabolism of anticoagulants and can increase effect of azathioprine and cyclophosphamide.
Colchicine
Anti-inflammatory
Actions: decreases pain and inflammation in gout
MOA: inhibits migration of neutrophils into gouty joints by binding to tubulin and preventing polymerisation into microtubules. Decreased chemokine leukotriene B4
Use: prevent and treat gout
SE: diarrhoea, nausea, vomiting.
Note - can increase bone marrow suppression caused by other drugs.
Lidocaine
Class 1B antidysrhythmic
Actions: antidysrhythmic, local anaesthetic
MOA: Blocks open and inactivated Na channels in cell membranes. more lilkely to act in damaged or depolarised tissue. Na channel black reduces the rate of phase 0 depolarisation, increasing refractory period and slowing AV conduction.
Use: Treatment and prevention of VF following infarction. Digoxin induced arrhythmias. Local anaesthetic.
SE: unwanted CNS effects - drowsiness, tremors, convulsions.
Flecanide
Class Ic antidysrhythmic
Actions: antidysrhythmic
MOA: Class Ic. Preferential block of Na channels. Reduces rate of phase 0 depolarisation causing an increase in effective refractory period and slowed AV conduction. Associates with and dissociates from sodium channels more slowly than 1a or 1b.
Use: Prevention of paroxysmal AF. Severe ventricular dysrhythmia, unresponsive to other agents
SE: Increased likelihood of dysrhythmia, May increase mortality due to VF post infarction. Avoid in patients with structural heart disease. Negative inotropic action.
Amiodarone
Class III antidysrhythmic, with some class I and II actions.
Actions: antidysrhythmic
MOA: Class III drugs block K+ channels in the cell membrane to delay repolarisation and increase potential duration. Increases refractory period. Also blocks Na channels and Beta adrenoceptors so has class I and class II actions.
Use: one of the most effective antidysrhythmics. AF, flutter, ventricular ectopics, tachyarrhythmias.
SE: torsades de pointes. Pulmonary fibrosis. Liver damage. Photosensitive skin rashes. Thyroid malfunction.
Sotalol
Antidysrhythmic- Class III with some class II actions
Action: antidysrhythmic.
MOA: class III drugs block K+ channels in the cell membrane to delay repolarisation and increase action potential duration. Increases refractory period. Has class II actions.
Use: effective antidysrhythmic. AF and flutter. Ventricular ectopic.
SE: Torsades de pointes.
Adenosine
Antidysrhythmic
Actions: antidysrhythmic
MOA: Activates G protein coupled adenosine receptors. Actions is due to inhibition of Ca 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 due to rapid elimination of adenosine.
Magnesium sulphate
Antidysrhythmic
Actions: antidysrhythmic. osmotic purgative.
MOA: Slows AV node conduction. Reduces increased cardiac excitability due to hypomagnesaemia which is common after heart operations. Cellular MOA not established.
Use: prevention of supraclavicular tachycardia and ventricular arrhythmias after bypass surgery. Ventricular dysrhythmias due to digoxin toxicity. management of torsades de pointes.
SE: muscle weakness.
Digoxin
Cardiac stimulant
Actions: slows heart. Slows AV conduction. Prolongs AV node refractory period. Increased force of contraction in failing heart.
MOA: Inhibits Na/K ATPase in plasma membrane. Increased intracellular Na reduces Ca extrusion increasing Ca++
Use: AF. Heart failure (if diuretics and ACEi have not worked)
SE: dysrhythmias, due to block of AV conduction and ectopic pacemaker action. Yellow vision. Nausea and vomiting.
NOTE: narrow margin for effective and therapeutic dose. Hypokalaemia increased toxicity due to competition between K+ and digoxin for Na/K ATPase
Clopidogrel
ANTIPLATELET antithrombotic drug
Actions: prevents platelet activation.
MOA: irreversibly inhibits the binding of ADP purine receptor on platelets thus inhibiting ADP mediated platelet activation and interfering with GpIIb/IIIa mediated platelet aggregation
Use: prevention and treatment of MI and other vascular disorders. Often given with aspirin.
SE: bleeding, GI discomfort, rashes. Rarely neutropaenia.
NOTE: effects increased by other antithrombotic drugs. Inhibits metabolism of NSAIDs and phenytoin.
Dipyridamole
Antiplatelet antithrombotic drug
Actions: inhibits platelet aggregation
MOA: has vasodilator activity. prevents platelet adenosine uptake and cyclic GMP phosphodiesterase action.
Use: used with aspirin for secondary prevention of stroke and TIA
SE: headache, GI disturbances, hypotension, hypersensitivity.
Alteplase
Thrombolytic drug
Actions & MOA: enzymatically activates plasminogen to give plasmin which digests fibrin and fibrinogen, lysing the clot.
Use: MI, DVT, PE, acute ischaemic stroke
SE: Bleeding, reperfusion dysrhythmias, nausea and vomiting, hypersensitivity reactions
NOTE: needs to be given within 12 hours, preferably within one hour.
Tenecteplase
Thrombolytic drug
Actions & MOA: enzymatically activates plasminogen to give plasmin which digests fibrin and fibrinogen, lysing the clot.
Use: MI, DVT, PE, acute ischaemic stroke
SE: Bleeding, reperfusion dysrhythmias, nausea and vomiting, hypersensitivity reactions
NOTE: needs to be given within 12 hours, preferably within one hour.
Folic acid
Haemotinic agent
Actions & MOA: folic acid is essential for DNA synthesis and cell proliferation. In the tetrahydrofolate FH4 form, it is a cofactor for the synthesis of purines and pyramidines
Use: treat megaloblastic anaemia caused by folate deficiency. Prevent folate deficiency in pregnancy, premature infants. Treat toxicity caused by methotrexate.
SE: rare. occasionally GIT disturbance.
NOTE: should not be used in undiagnosed megaloblastic anaemias.
Hydroxycobalamin
B12 vitamin preparation
Actions: restores the blood picture in megaloblastic anaemia (pernicious). Results in partial to full recovery of the neurological syndrome.
MOA: necessary for conversion of methyl-tetrahydrofolate (methyl FH4) to FH4 which is essential for thymidylate synthesis and thus for DNA synthesis.
Use: treat pernicious anaemia and other causes of B12 deficiency.
SE: nausea, dizziness, headache, hypersensitivity reactions. Hypokalaemia at start of treatment.
Darbepoetin
Actions: binds to receptors on committed erythrocyte progenitor cells stimulating proliferation and differentiation
Use: treat anaemia of chronic renal failure and AIDS. to alleviate anaemia caused by cytotoxic anticancer drugs. Prevent anaemia is premature infants.
SE: GIT disturbance. hypertension.
Ferrous sulphate
Haemotinic agent
Actions & MOA: used in haemoglobin production in red blood cell precursors in the bone marrow.
Use: iron deficiency anaemia.
SE: dose related GIT disturbances. Nausea, epigastric pain, abdominal cramps, diarrhoea
NOTE: iron toxicity both acute or chronic is treated with desferrioxamine.
Ferrous fumarate, ferrous gluconate.
Theophylline
XANTHINE
Actions: bronchodilation.
MOA: inhibits phosphodiesterase PDE4 and increasing cAMP and relaxing smooth muscle. Inhibition of PDE4 in inflammatory cells can decrease mediator release.
Use: chronic asthma not adequately controlled.
SE: GIT disturbances, tachycardia, anxiety/ high plasma levels can cause serious dysrhythmia or seizures.
Need to monitor plasma levels.
Aminophylline
XANTHINE
Actions: bronchodilation.
MOA: inhibits phosphodiesterase PDE4 and increasing cAMP and relaxing smooth muscle. Inhibition of PDE4 in inflammatory cells can decrease mediator release.
Use: chronic asthma not adequately controlled. acute asthma attack.
SE: GIT disturbances, tachycardia, anxiety/ high plasma levels can cause serious dysrhythmia or seizures.
Need to monitor plasma levels.
Montelukast
Leukotriene receptor antagonist
Actions: reverses bronchoconstriction. Relaxes airway smooth muscle in mild asthma.
MOA: drug is antagonist at cysteinyl leukotriene receptor, on which the bronchospasmic mediators LTc4, LTD4. LTE4. It can decrease the early and late phase response to inhaled allergen.
Use: asthma, used as adjunct to inhaled corticosteroids. Effective in aspirin induced asthma.
SE: Few
Ipratropium
Muscarinic receptor antagonist
Actions: bronchodilation by inhibiting acetylcholine-mediated bronchoconstriction and mucus secretion. No effect on late phase.
MOA; competitively antagonises acetylcholine action on muscarinic receptors.
Use: for asthma as adjunct therapy. COPD
SE: Few
Tiotropium
Muscarinic receptor antagonist
Actions: bronchodilation by inhibiting acetylcholine-mediated bronchoconstriction and mucus secretion. No effect on late phase.
MOA; competitively antagonises acetylcholine action on muscarinic receptors.
Use: for asthma as adjunct therapy. COPD
SE: Few
Beclometasone
Corticosteroid
Actions: reduces hyper-reactivity and decreases the inflammatory delayed phase. No effect on immediate phase.
MOA: reduces the activation of inflammatory cells and release of mediatory especially cytokines.
Use: added to bronchodilator therapy if inadequate. IV hydrocortisone is life saving in acute severe asthma
SE: hoarse voice. oral candidiasis.
NOTE: regular high doses can cause adrenal suppression and other adverse effects.
Fluticasone
Corticosteroid
Actions: reduces hyper-reactivity and decreases the inflammatory delayed phase. No effect on immediate phase.
MOA: reduces the activation of inflammatory cells and release of mediatory especially cytokines.
Use: added to bronchodilator therapy if inadequate. IV hydrocortisone is life saving in acute severe asthma
SE: hoarse voice. oral candidiasis.
NOTE: regular high doses can cause adrenal suppression and other adverse effects.
Cromoglicate
Prophylactic antiasthma drug
Actions: moderate inhibition of allergen. Exercise induced asthma and bronchial hyper-reactivity. No effect on bronchial spasm.
MOA: inhibits mast cell degranulation and response of sensory C fibres to irritants (early phase) and eosinophil activation (delayed phase) possibly by and action on chloride channels in plasma membrane.
Use: prophylaxis of asthma, mainly in older children. Recues symptoms of allergic rhinitis.
SE: irritation of throat by powder.
Aluminium hydroxide
Antacid
Actions: raised pH in gut lumen
MOA: antacids are weak bases that neutralise the HCl secreted in the stomach. Elevation of pH also usefully reduces the activity of pepsin. Stimulates prostaglandin synthesis.
Use: short term relief for duodenal ulcers. GORD.
5-7 times daily
SE: constipation, strong laxative actions. Metabolic alkalosis.
Prevent absorption of tetracyclines.
Hydrocortisone
Anti-inflammatory / immunosuppressant glucocorticoid
Actions: reduction in chronic inflammation and in autoimmune and hypersensitivity reactions. Decrease uptake and utilisation of glucose. Gluconeogenesis. Decreased protein synthesis.
MOA: interact with intracellular receptors that control transcription of specific genes.
Use: inflammatory, hypersensitivity and autoimmune disease (RA, asthma, anaphylaxis), prevent graft rejection. Replacement therapy in adrenal failure.
SE: suppression of immune system, suppression of endogenous GC synthesis. osteoporosis. growth suppression in children. cushings
Fludrocortisone
Mineralocorticoid - regulating water and electrolyte balance
Actions: acts on distal renal tubule to increase Na+ reabsorption and increase excretion of K+ and H+
MOA: interact with intracellular receptors in the kidney controlling transcription of specific genes.
Increased number of Na channels
Increased number of Na pumps
Use: used with a glucocorticoid for replacement therapy in adrenal insufficiency
SE: hypokalaemia. increased by thiazide or loop diuretics.
Carbimazole
Anti-thyroid drug - thyroid peroxidase inhibitor
Actions: gradually decreases thyroid hormone output and thus reduces signs and symptoms of thyrotoxicosis
MOA; reduces the synthesis of thyroid hormone by inhibiting thyroperoxidase which normally iodinates tyrosyl residues in thyroglobulin to give the precursors T3 and T4.
Use: hyperthyroidism.
SE: agranulocytosis. Rashes. Joint pains.
Note: response can take several weeks as thyroid stores of hormone need to be depleted.
Levothyroxine
Synthetic T4
Actions: increased metabolism of carbohydrates, fats and proteins. Increase in basal metabolic rate.
MOA: drug enters cells and is converted to T3 which enters the nucleus and binds to the thyroid hormone receptor. The complex activates transcription resulting in generation of mRNA and synthesis of proteins and enzymes responsible for metabolic actions of T4.
Use: hypothyroidism.
SE: nervousness, palpitations, insomnia, heat intolerance, weight loss.
NOTE; best given on empty stomach as it can interfere with absorption.
Radioactive iodine
131 I
MOA: emits both x-rays (which do not do any damage) and beta radiation which has a very short range and is cytotoxic to local thyroid cells
ADE: given orally as a single dose, taken up by thyroid cells, incorporated into thyroglobulin
Use: thyrotoxicosis. Maximum effect takes approx. 4 months
SE: hypothyroidism will eventually occur.
Raloxifene
Selective Oestrogen receptor modulator (SERM)
Actions: agonist effects on bone and on CVS but antagonist action on mammary glands and uterus
MOA: like the oestrogens, inhibits the cytokines that recruit osteoclasts.
Use: prophylaxis for postmenopausal osteoporosis and breast cancer.
SE: risk of VTE
Ethinylestradiol & Norethisterone
Actions and use: prevention of pregnancy
MOA: ethinylestradiol suppresses the development of ovarian follicle by inhibiting FSH release from anterior pituitary. Norethisterone prevents ovulation by inhibiting LH release.
SE: infrequent. Weight gain, flushing, mood changes, dizziness, acne, transient rise in BP. Risk of VTE
Combinations:
- ethinylestradiol and desogestrel
- Ethinylestradiol and drospirenone
COCP brand names
Gedarel - ethinylestradiol + desogestrel
Mercilon - ethinylestradiol + desogestrel
Yasmin - ethinylestradiol + drospirenone
Femodene - ethinylestradiol + gestodene
Cilest - ethinylestradiol + norgestimate
Microgynon - ethinylestradiol + levonorgestrel
Oxytocin
Uterine stimulant - oxytocin
Actions: contract uterus causing co-ordinated contractions that travel from fundus to cervix with complete relaxation between contractions.
MOA: acts on oxytocin receptors in smooth muscle of myometrium
Use: induce or augment labour when the uterine muscle not functioning adequately.
Prevent or treat PPH from uterine atony.
Treat haemorrhage due to incomplete abortion
SE: hypotension due to vasodilation. Water retention.
NOTE: contracts myoepithelial cells in post-partum mammary gland causing milk let down
Syncometrine
Uterine stimulant
Actions: contract uterus causing co-ordinated contractions that travel from fundus to cervix with complete relaxation between contractions.
MOA: acts on oxytocin receptors in smooth muscle of myometrium
Use: induce or augment labour when the uterine muscle not functioning adequately.
Prevent or treat PPH from uterine atony.
Treat haemorrhage due to incomplete abortion
SE: hypotension due to vasodilation. Water retention.
NOTE: contracts myoepithelial cells in post-partum mammary gland causing milk let down
Ergometrine
Uterine stimulant
Actions: contracts the relaxes uterus. Has vasoconstrictor action.
MOA: Not understood. may act partly on alpha adrenoceptors, partly on 5HT receptors.
Use: Treat PPH
SE: GIT disturbance, increase in BP, headache, dizziness, dysrhythmias.
Carboprost
PGF 2alpha analogue - uterine stimulant
Actions: causes coordinated contractions of pregnant uterus, relaxes the cervix
MOA: activates PGF-2alpha receptors on uterine smooth muscle.
Use: treat PPH unresponsive to oxytocin or ergometrine.
SE: GIT disturbances, bronchospasm, fever. sometimes dizziness, headache, hypertension.
Atosiban
Oxytocin antagonist
Actions: inhibits oxytocin induced contractions of the pregnant uterus.
MOA: antagonises oxytocin action on oxytocin action on oxytocin receptors on uterine smooth muscle causing relaxation.
Use: to delay pre-term labour
SE: GIT disturbances, tachycardia, hypotension, dizziness, headache
Finasteride
Inhibits 5 alpha reductase.
5 alpha reductase converts testosterone to dihydrotestoterone which has greater affinity for the androgen receptor.
Use: BPH. Alpha blockers are more effective.
SE: erectile dysfunction, libido loss.
Sildenafil
Enhances penile erection
Actions: relaxes non-vascular smooth muscle of corpora cavernosa. Blood at virtually arterial pressure flows into cavenosa sinuses resulting in swelling and erection of the penis.
MOAL: Inhibits phosphodiesterase type V. enzyme normally converts cGMMP to 5-GMP. This increases the concentration of cGMP which inhibits contractile mechanisms of the muscle allowing relaxation.
Use: erectile dysfunction
SE: due to action of the drug on other vascular beds. headache, hypotension, flushing.
Tadalafil
Enhances penile erection
Actions: relaxes non-vascular smooth muscle of corpora cavernosa. Blood at virtually arterial pressure flows into cavenosa sinuses resulting in swelling and erection of the penis.
MOAL: Inhibits phosphodiesterase type V. enzyme normally converts cGMMP to 5-GMP. This increases the concentration of cGMP which inhibits contractile mechanisms of the muscle allowing relaxation.
Use: erectile dysfunction
SE: due to action of the drug on other vascular beds. headache, hypotension, flushing.
Levodopa
Precursor of dopamine
Action: antiparkinsonian
MOA: decarboxylation of levodopa to dopamine restores some activity in nigrostriatal pathway.
Use: Parkinson’s disease. Usually given with a peripheral DOPA decarboxylase inhibitior.
SE:
Effectiveness dimishes with time - can be months or years.
SE: anorexia, nausea, vomiting, postural hypotension. Acute schizophrenia like syndrome. Confusion, anxiety, disorientation, insomnia, nightmares.
Dyskinesia
Carbidopa
Peripheral DOPA decarboxylase inhibitor
Actions: antiparkinsonian
MOA: inhibits levodopa decarboxylation outside the brain, allowing the use of smaller doses and reducing peripheral side effects.
Use: Parkinson’s disease - used with levodopa
SE: anorexia, nausea and vomiting. Postural hypotension, confusion, anxiety, disorientation, insomnia, nightmares
Dyskinesia
Benserazide
Peripheral DOPA decarboxylase inhibitor
Actions: antiparkinsonian
MOA: inhibits levodopa decarboxylation outside the brain, allowing the use of smaller doses and reducing peripheral side effects.
Use: Parkinson’s disease - used with levodopa
SE: anorexia, nausea and vomiting. Postural hypotension, confusion, anxiety, disorientation, insomnia, nightmares
Dyskinesia
Entacapone
Catechol-O-methyl transferase inhibitor
Actions: Synergises with antiparkinsonian effects of levodopa/carbidopa. Potentiates actions of catecholamines
MOA: reversible inhibition of COMT in periphery reduces levodopa breakdown, allowing more of levodopa dose to penetrate brain.
Use: adjunct to levodopa/carbidopa therapy - especially for patients showing end of dose symptoms
No antiparkinsonian effect by itself.
SE: exacerbates adverse effects of levodopa/carbidopa taken at the same time.
Dyskinesia, nausea, diarrhoea, postural hypotension, hallucinations, anxiety and sleepiness.
Morphine
Opiate receptor agonist
Actions: analgesia. Sedation. Euphoria. decreases anxiety. Dependence. Cough and respiratory depression. Inhibition of gut motility
MOA: Activates mu opioid receptors in brain and spinal cord to inhibit pain transmission.
Use: moderate to severe chronic and post-op pain
Epidural anaesthesia, neuropathic pain. painful cough. diarrhoea
Side effects: hypotension. constipation. nausea. vomiting. drowsiness. tolerance. dependence. withdrawal
OD = coma and respiratory depression
Diamorphine
Opiate receptor agonist
Actions: analgesia. Sedation. Euphoria. decreases anxiety. Dependence. Cough and respiratory depression. Inhibition of gut motility
MOA: Activates mu opioid receptors in brain and spinal cord to inhibit pain transmission.
Diamorphine metabolised into morphine
Use: moderate to severe chronic and post-op pain
Epidural anaesthesia, neuropathic pain. painful cough. diarrhoea
Side effects: hypotension. constipation. nausea. vomiting. drowsiness. tolerance. dependence. withdrawal
OD = coma and respiratory depression
Codeine
Opiate receptor agonist
Actions: analgesia. Sedation. Euphoria. decreases anxiety. Dependence. Cough and respiratory depression. Inhibition of gut motility
MOA: Activates mu opioid receptors in brain and spinal cord to inhibit pain transmission.
Use: moderate to severe chronic and post-op pain
Epidural anaesthesia, neuropathic pain. painful cough. diarrhoea
Side effects: hypotension. constipation. nausea. vomiting. drowsiness. tolerance. dependence. withdrawal
OD = coma and respiratory depression
Fentanyl
Opioid receptor agonist
Actions: analgesia. euphoria. dependence. resp depression. decreased gut motility
MOA: Activates mu opioid receptors (as morphine)
Available as transdermal patch for long term effects
Use: moderate to severe pain. Doesn’t give uterine contractions (labour pain). surgical anaesthesia.
Side effects: constipation (less than morphine), hypotension. . nausea. vomiting. drowsiness. tolerance. dependence. withdrawal
Pethidine
Opioid receptor agonist
Actions: analgesia. euphoria. dependence. resp depression. decreased gut motility
MOA: Activates mu opioid receptors (as morphine)
Available as transdermal patch for long term effects
Use: moderate to severe pain. Doesn’t give uterine contractions (labour pain). surgical anaesthesia.
Side effects: constipation (less than morphine), hypotension. . nausea. vomiting. drowsiness. tolerance. dependence. withdrawal
Tramadol
Atypical narcotic analgesic
Actions: analgesia
MOA; weak agonist at mu opioid receptors. Main action due to the enhancement of monoamine neurotransmission by inhibiting 5HT and Na uptake into nerve endings. Analgesia from 5HT3 receptor antganosit
Use: moderate pain, post-op pain, neuropathic pain
Side effects: dizziness, N&V, respiratory depression, constipation and addiction (less than morphine). Convulsions
Celecoxib
COX2 selective NSAID
Actions: anti-inflammatory. analgesic
MOA: Inhibits cyclo-oxygenase iso-enzymes. Inhibit the production of prostaglandins at the site and prevents increased sensitivity of pain receptors.
Use: mild-moderate pain due to inflammatory disease.
Side effects: Increased CV risk (MI and stroke). less GIT bleeding and ulceration than COX1
Anastrazole
AROMATASE INHIBITOR
Actions and MOA: inhibits oestrogen synthesis. Aromatase inhibitor. Aromatase converts precursors (testosterone and androstenedione) into oestrogen.
Use: Oestrogen receptor positive breast cancers AFTER menopause
Side effects: numbness, tinging of the hands, hot flashes, joint pain, sleep problems, N&V, hair thinning
Flurouracil
ANTIMETABOLITE
Actions: interferes with the synthesis of dTMP and with DNA synthesis
MOA; gives rise to a fraudulent nucleotide and inhibits thymidylate synthase
Use: Cancers of GIT, pancreas, breast, malignant skin conditions
Side effect: myelosuprression, GIT disturbance, mucositis.
Cytarabine
ANTIMETABOLITE
Actions and MOA: pyramidine analogue that is converted in the cell to triphosphate which inhibits DNA polymerase
Use: AML
Side effects: marked myelosuppression. GIT disturbance, cerebellar ataxia
Bleomycin
Cytotoxic antibiotic/ anticancer agent
Actions: causes DNA fragmentation
Use: Squamous cell cancer. metastatic germ cell. Non-Hodgkin’s lymphoma
Side effects: PULMONARY FIBROSIS, skin toxicity, mucositis, transient hypersensitivity reactions. minimal myelosuppression
Cisplatin
CYTOTOXIC
Actions/MOA: forms a reactive complex that causes intrastrand CROSSLINKING and denaturation of DNA
Use: cancer of testes, ovaries, cervix, bladder, lung, head and neck
SE: nephro/oto toxic, severe nausea and vomiting, myelosuppression, peripheral neuropathy, hypomagesaemia
Carboplatin
CYTOTOXIC
Actions/MOA: forms a reactive complex that causes intrastrand CROSSLINKING and denaturation of DNA
Use: cancer of testes, ovaries, cervix, bladder, lung, head and neck
SE: nephro/oto toxic, severe nausea and vomiting, myelosuppression, peripheral neuropathy, hypomagesaemia
Myelosuprresion is greater than cisplatin but other side effects reduced
Cyclophosphamide
ALKYLATING AGENT
Actions: cross links DNA by forming covalent bonds with guanine residues on each strand. interferes with cell division and triggering apoptosis.
Use: CLL, soft tissue sarcoma, osteogenic sarcoma, ovarian and breast cancer
SE: nausea and vomiting. myelosuppression, alopecia, infertility, leukaemia
Doxorubicin
CYTOTOXIC
Actions: inhibits DNA and RNA synthesis through an effect on topoisomerase II
Use: acute leukaemias, Hodgkin’s and non-Hodgkin’s lymphoma, tumours of breast, ovary, bladder, bronchi
SE: dose related cardiac damage. nausea and vomiting, hair loss, myelosuppression
Vincristine
Vinca Alkaloid
Actions and MOA: binds to tubulin preventing spindle formation in dividing cells stopping them in mitosis
Use; leukaemia, lymphoma, breast and lung cancers
SE: nausea and vomiting, hair loss, neurotoxicity,
Paclitaxel
Anticancer
Actions and MOA: binds to tubulin, keeping microtubules polymerised , preventing spindle formation in dividing cells and stopping them in mitosis
Use: ovary and breast cancer. non small cell lung cancer
SE: hypersensitivity reactions, myelosuppression, peripheral neuropathy, bradycardia, muscle and joint pain
Imatinib
Protein kinase inhibitor
Actions and MOA: inhibits protein kinases important in CML and other malignancies
Use: CML, ALL, myeloproliferative disease,
SE: GIT disturbance, abdo pain, oedema, haemorrhage, cough, dyspnoea, paraesthesia, arthralgia, photosensitivity, headache, dizziness, sweating, rash
Trastuzumab
Herceptin/ monoclonal antibody
Actions: binds to and inhibits epidermal growth factor receptor (tyrosine kinase receptor) preventing it’s activation and inhibiting cell proliferation
Use: HER2 positive breast cancers
SE: GI disturbance, hypersensitivity, cardiac toxicity, paraesthesia, headache, dizziness, anxiety, depression, oedema, arthralgia
Tamoxifen
Selective oestrogen receptor modulator (SERM)
Actions and MOA; oestrogen receptor AGONIST. Competes with endogenous oestrogen for oestrogen receptor preventing cell activation and proliferation
Use: Oestrogen receptor positive breast cancer
SE: hot flushes, GIT disturbance, headache, menstrual irregularities
NOTE: only used in premenopausal women
