Block 1 Flashcards

1
Q

Antacids

A
  • Used to treat disorders of gastric acid secretion
  • Generic drug names: aluminium hydroxide and magnesium hydroxide, calcium carbonate and magnesium carbonate
  • Mechanism of action: gastric acid neutralisation
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2
Q

Antacids + alginates

A
  • Used to treat disorders of gastric acid secretion
  • Generic drug names: sodium alginate with sodium bicarbonate and calcium carbonate
  • Mechanism of action: gastric acid neutralisation and increasing viscosity of stomach contents
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3
Q

H2 receptor antagonists

A
  • Used to treat disorders of gastric acid secretion
  • Generic drug names: famotidine
  • Mechanism of action: blockade of gastric H2 histamine receptors
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4
Q

Proton pump inhibitors

A
  • Used to treat disorders of gastric acid secretion
  • Generic drug names: omeprazole, lansoprazole
  • Mechanism of action: blockade of parietal cell proton transporters
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5
Q

Bulk laxatives

A
  • A purgative
  • Generic drug names: methylcellulose, ispaghula husk
  • Mechanism of action: increases water retention in intestinal lumen to soften & increase bulk of stools. Bulkier stools drive colonic distention which stimulates intestinal motility.
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6
Q

Osmotic laxatives

A
  • A purgative
  • Generic drug names: magnesium sulphate and magnesium hydroxide (saline purgatives), macrogol, lactulose
  • Mechanism of action: promotes the movement of fluid across the wall into the GI lumen, which accelerates transit and causes colonic distension, simulating transit and purgation
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7
Q

Faecal softeners

A
  • A purgative
  • Generic drug names: docusate (docusate sodium), arachis oil
  • Mechanism of action: this lowers the surface tension, allowing water and fat to enter stool, softening stool consistency & increasing stool size to promote transit and purgation
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8
Q

Stimulant purgatives

A
  • A purgative
  • Generic drug names: bisacodyl, senna
  • Mechanism of action: stimulates increased intestinal motility
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9
Q

Oral rehydration therapy

A

-Used in the treatment of diarrhoea
-Generic drug names: isotonic/hypotonic solution of glucose and sodium chloride
-Mechanism of action: promotes uptake of Na+ and water by intestines, restoring
hydration levels following fluid loss from diarrhoea

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10
Q

Opioid anti-motility agents

A
  • Used in the treatment of diarrhoea
  • Generic drug names: loperamide, codeine
  • Mechanism of action: agonist for µ-opioid receptors in myenteric plexus, reducing intestinal motility
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11
Q

Aminosalicylate (for inflammatory bowel disease)

A
  • Used in the treatment for diarrhoea
  • Generic drug names: mesalazine
  • Mechanism of action: suppresses immune system in the gut to reduce inflammation and tissue damage
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12
Q

Loop diuretics

A
  • A diuretic
  • Generic drug names: furosemide
  • Mechanism of action: inhibits Na+/K+/2Cl- transporter in loop of Henle
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13
Q

Thiazides (& thiazide-like drugs)

A
  • A diuretic
  • Generic drug names: indapamide, bendroflumethiazide, hydrochlorothiazide, chlortalidone
  • Mechanism of action: inhibits Na+/Cl- co-transporter in early distal tubule
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14
Q

Potassium-sparing diuretics

A
  • Diuretic
  • Generic drug names: spironolactone, eplerenone (mineralocorticoid receptor antagonist class)
  • Mechanism of action for spironolactone and eplerenine: blockade of mineralocorticoid receptor
  • Generic drug names: amiloride (epithelial sodium channel (ENaC) antagonist)
  • Mechanism of action for amiloride: blockade of sodium reabsorption via ENaC channel
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15
Q

Angiotensin Converting Enzyme (ACE) inhibitors

A
  • Drugs which affect the renin-angiotensin-aldosterone system
  • Generic drug names: Ramipril, lisinopril
  • Mechanism of action: inhibits conversion of angiotensin I to angiotensin II and reduces vasoconstriction
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16
Q

Angiotensin-II receptor antagonists

A
  • Drugs which affect the renin-angiotensin-aldosterone system
  • Generic drug names: losartan
  • Mechanism of action: blockade of cell signalling induced by angiotensin II receptors, and this reduces vasoconstriction
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17
Q

Aldosterone antagonist

A
  • Drugs which affect the renin-angiotensin-aldosterone system
  • Generic drug name: spironolactone, eplerenone
  • Mechanism of action: blockade of mineralocorticoid receptor activation
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18
Q

Thyroid hormones

A
  • Drugs used to treat thyroid disorders
  • Generic drug names: levothyroxine, liothyronine
  • Mechanism of action: activation of thyroid hormone receptors
19
Q

Alpha-adrenergic antagonists (for urinary retention)

A
  • Used to treat altered voiding
  • Generic drug name: tamsulosin
  • Mechanism of action: smooth muscle relaxant affecting neck of bladder to promote the passage of urine
20
Q

Antimuscarinic class (used to treat urinary incontinence)

A
  • Used to treat altered voiding
  • Generic drug name: oxybutinin
  • Mechanism of action: blockade of muscarinic acetylcholine receptors leading to relaxation of bladder detrusor muscle to promote holding of urine
21
Q

What are the common routes of drug administration?

A
  • Intravenous injection
  • Oral route
  • Mucosal route
  • Inhalation route
  • Transdermal route
  • Subcutaneous route
  • Intramuscular route
22
Q

What is pharmacokinetics?

A

This is the study of drug movement within the body - what the body does to a drug.

23
Q

What are the 4 phases of pharmacokinetics?

A
  • Absorption
  • Distribution
  • Metabolism - conversion of drugs to inactive compounds; or inactive pro-drugs becoming active drugs; active metabolites
  • Elimination
24
Q

What do we know about drug metabolism?

A
  • The liver is the major site of drug metabolism
  • Orally administered drugs, absorbed by the GIT, are transported via the portal system through the liver where they are metabolised to an extent before entering the systemic circulation. This is first pass metabolism.
  • A drug may pass through the liver many times because of continual systemic blood circulation
  • Each time a drug passes through the liver, a fraction of it is metabolised
  • Molecules of metabolised drugs are excreted out of the body either via kidneys or through the bile.
25
Q

3 phases of drug metabolism

A
  • Phase 1: drug to intermediate metabolite - can be oxidation which occurs by cytochrome P450, reduction or hydrolysis
  • Phase 2: drug or intermediate metabolite to conjugated metabolite
  • Phase 3: conjugated metabolite to excretion via the kidney or bile.
26
Q

What are the cytochrome P450 enzymes?

A
  • A superfamily of enzymes located on SER
  • Several hundred isoforms exist - examples are CYP3A, CYP2D6, CYP2CP, CYP1A2.
  • Some are constitutive, some are inducible
27
Q

What is conjugation - give an example?

A
28
Q

What are the effects of age on drug metabolism?

A
29
Q

What is cimetidine?

A

Cimetidine is a histamine H2 receptor antagonist This is an inhibitor of many CYP450 enzymes and it reduces the metabolism of endogenous steroids and co-administered drugs such as warfarin, phenytoin and quinidine. Plasma levels of these drugs will therefore be elevated and biological effects increased. This can cause potentially toxic drug levels and adverse effects.

30
Q

How can omeprazole be inactivated?

A
31
Q

How can codeine be activated?

A
32
Q

What are poor metabolisers?

A
33
Q

What are ultra-rapid metabolisers?

A
34
Q

What is opioid toxicity?

A
35
Q

What is bioavailability?

A
36
Q

What can cause hypoproteinaemia?

A
37
Q

What is constipation?

A
38
Q

What causes constipation?

A
39
Q

What is a cathartic colon?

A
40
Q

How can constipation be prevented?

A
41
Q

What is diarrhoea?

A
42
Q

What are the different types of diarrhoea?

A
43
Q

What are anti-infective agents?

A