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Year 3 > PPT > Flashcards

PPT Flashcards

1
Q

Amitriptyline

A

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
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2
Q

Imipramine

A

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
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3
Q

Lofepramine

A

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
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4
Q

Citalopram

A

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
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5
Q

Fluoxetine

A

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
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6
Q

Sertraline

A

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
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7
Q

Paroxetine

A

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
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8
Q

Duloxetine

A

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
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9
Q

Venlafaxine

A

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
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10
Q

Reboxetine

A

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
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11
Q

Phenelzine

A

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
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12
Q

Moclobemine

A

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
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13
Q

Isocarboazid

A

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
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14
Q

Mirtazipine

A

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)

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15
Q

Bupropion

A

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

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16
Q

Mesalazine

A

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

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17
Q

Prednisolone

A

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

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18
Q

Budesonide

A

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

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19
Q

Ciclosporin

A

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

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20
Q

Azathioprine

A

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

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21
Q

Mercaptopurine

A

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

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22
Q

Infliximab

A

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

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23
Q

Omeprazole

A

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

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24
Q

Lansoprazole

A

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

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25
Q

Ranitidine

A

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

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26
Q

Cimetidine

A

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

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27
Q

Terlipressin

A

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

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28
Q

Loperamide

A

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.

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29
Q

Investigations for chronic diarrhoea

A

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
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30
Q

Macrogol

A

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

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31
Q

Lactulose

A

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

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32
Q

Lubiprostone

A

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.

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33
Q

Docusate

A

STOOL SOFTENER

Actions: softens and lubricates the stool to allow easier passage

MOA: surfactant with emulsifying action

Use: constipation and haemorrhoids

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34
Q

Methylcellulose

A

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

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35
Q

Ispaghula husk

A

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

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36
Q

Bisacodyl

A

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

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37
Q

Senna

A

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

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38
Q

Hyoscine

A

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

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39
Q

Atropine

A

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

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40
Q

Metronidazole

A

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

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41
Q

Ramipril

A

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

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42
Q

Losartan

A

ARB

Actions: Lowers BP by decreasing vasoconstrictor tone

MOA: Blocks action of angiotensin II

Use: hypertension. Congestive heart failure. Nephropathy

SE: hypotension, dizziness, hyperkalaemia

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43
Q

Lisinopril

A

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

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44
Q

Candesartan

A

ARB

Actions: Lowers BP by decreasing vasoconstrictor tone

MOA: Blocks action of angiotensin II

Use: hypertension. Congestive heart failure. Nephropathy

SE: hypotension, dizziness, hyperkalaemia

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45
Q

Glyceryl trinitrate

A

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.

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46
Q

Isosorbide dinitrate

A

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.

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47
Q

Furosemide

A

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

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48
Q

Bumetanide

A

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

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49
Q

Bendroflumethiazide

A

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

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50
Q

Metolazone

A

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

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51
Q

Spironolactone

A

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

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52
Q

Eplerenone

A

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

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53
Q

Bisoprolol

A

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

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54
Q

Carvedilol

A

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

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55
Q

Amiloride

A

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

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56
Q

Indapamide

A

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

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57
Q

Amlodipine

A

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

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58
Q

Nifedipine

A

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

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59
Q

Verapamil

A

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

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60
Q

Atenolol

A

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

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61
Q

Propranolol

A

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.

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62
Q

Metoprolol

A

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

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63
Q

Doxazosin

A

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

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64
Q

Tamsulosin

A

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

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65
Q

Diltiazem

A

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

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66
Q

Bendroflumethazide

A

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

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67
Q

Simvastatin

A

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)

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68
Q

Atorvastatin

A

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)

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69
Q

Gemfibrozil

A

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

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70
Q

Bezafibrate

A

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

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71
Q

Fenofibrate

A

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

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72
Q

Ezetimibe

A

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

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73
Q

Aspirin

A

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

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74
Q

LMWH

A

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
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75
Q

Dalteparin

A

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
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76
Q

Fondaparinux

A

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
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77
Q

Heparin

A

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

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78
Q

Warfarin

A

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
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79
Q

Rivaroxaban

A

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

80
Q

Dabigatran

A

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

81
Q

methotrexate

A

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

82
Q

Chlorpromazine

A

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

83
Q

Haloperidol

A

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
84
Q

Flupentixol

A

Typical antipsychotic

Action: antipsychotic. antidepressant

MOA: competitive antagonism of dopamine D2 receptors.

Use: schizophrenia. psychosis. bipolar disorders.

Side effects: EPS, hyperprolactinaemia, neuroleptic malignant syndrome

85
Q

Clozapine

A

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

86
Q

Olanzipine

A

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

87
Q

Risperidone

A

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

88
Q

Quetiapine

A

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
89
Q

Sulpiride

A

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

90
Q

Amisulpiride

A

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

91
Q

Aripiprazole

A

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.

92
Q

Lithium

A

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
93
Q

Carbamazepine

A

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

94
Q

Sodium valproate

A

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

95
Q

Insulin

A

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.

96
Q

Metformin

A

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

97
Q

Gliclazide

A

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

98
Q

Glimepiride

A

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

99
Q

Repaglinide

A

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

100
Q

Pioglitazone

A

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

101
Q

Acarbose

A

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

102
Q

Sitagliptin

A

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

103
Q

Linagliptin

A

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

104
Q

Canagliflozin

A

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

105
Q

Dapagliflozin

A

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

106
Q

Exenatide

A

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

107
Q

Liraglitide

A

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

108
Q

Empagliflozin

A

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

109
Q

Saxagliptin

A

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

110
Q

Bupropion

A

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

111
Q

Vareniciline

A

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

112
Q

Nicotine replacement therapy

A

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

113
Q

Suxamethonium

A

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.

114
Q

Succinylcholine

A

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.

115
Q

Pancuronium

A

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

116
Q

Vecuronium

A

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

117
Q

Rocuronium

A

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

118
Q

Atracurium

A

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

119
Q

Cisatricurium

A

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

120
Q

Mivacurium

A

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

121
Q

Neostigmine

A

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.

122
Q

Pyridostigmine

A

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.

123
Q

Edrophonium

A

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.

124
Q

Salbutamol

A

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.

125
Q

Terbutaline

A

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.

126
Q

Salmetrol

A

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.

127
Q

Ibuprofen

A

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.

128
Q

Naproxen

A

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.

129
Q

Paracetamol

A

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.

130
Q

Allopurinol

A

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.

131
Q

Colchicine

A

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.

132
Q

Lidocaine

A

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.

133
Q

Flecanide

A

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.

134
Q

Amiodarone

A

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.

135
Q

Sotalol

A

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.

136
Q

Adenosine

A

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.

137
Q

Magnesium sulphate

A

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.

138
Q

Digoxin

A

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

139
Q

Clopidogrel

A

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.

140
Q

Dipyridamole

A

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.

141
Q

Alteplase

A

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.

142
Q

Tenecteplase

A

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.

143
Q

Folic acid

A

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.

144
Q

Hydroxycobalamin

A

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.

145
Q

Darbepoetin

A

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.

146
Q

Ferrous sulphate

A

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.

147
Q

Theophylline

A

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.

148
Q

Aminophylline

A

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.

149
Q

Montelukast

A

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

150
Q

Ipratropium

A

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

151
Q

Tiotropium

A

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

152
Q

Beclometasone

A

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.

153
Q

Fluticasone

A

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.

154
Q

Cromoglicate

A

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.

155
Q

Aluminium hydroxide

A

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.

156
Q

Hydrocortisone

A

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

157
Q

Fludrocortisone

A

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.

158
Q

Carbimazole

A

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.

159
Q

Levothyroxine

A

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.

160
Q

Radioactive iodine

A

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.

161
Q

Raloxifene

A

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

162
Q

Ethinylestradiol & Norethisterone

A

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
163
Q

COCP brand names

A

Gedarel - ethinylestradiol + desogestrel

Mercilon - ethinylestradiol + desogestrel

Yasmin - ethinylestradiol + drospirenone

Femodene - ethinylestradiol + gestodene

Cilest - ethinylestradiol + norgestimate

Microgynon - ethinylestradiol + levonorgestrel

164
Q

Oxytocin

A

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

165
Q

Syncometrine

A

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

166
Q

Ergometrine

A

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.

167
Q

Carboprost

A

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.

168
Q

Atosiban

A

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

169
Q

Finasteride

A

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.

170
Q

Sildenafil

A

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.

171
Q

Tadalafil

A

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.

172
Q

Levodopa

A

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

173
Q

Carbidopa

A

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

174
Q

Benserazide

A

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

175
Q

Entacapone

A

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.

176
Q

Morphine

A

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

177
Q

Diamorphine

A

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

178
Q

Codeine

A

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

179
Q

Fentanyl

A

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

180
Q

Pethidine

A

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

181
Q

Tramadol

A

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

182
Q

Celecoxib

A

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

183
Q

Anastrazole

A

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

184
Q

Flurouracil

A

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.

185
Q

Cytarabine

A

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

186
Q

Bleomycin

A

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

187
Q

Cisplatin

A

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

188
Q

Carboplatin

A

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

189
Q

Cyclophosphamide

A

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

190
Q

Doxorubicin

A

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

191
Q

Vincristine

A

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,

192
Q

Paclitaxel

A

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

193
Q

Imatinib

A

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

194
Q

Trastuzumab

A

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

195
Q

Tamoxifen

A

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

Year 3 (6 decks)

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