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Foundations Of Medicine 1 > Core Drugs > Flashcards

Core Drugs Flashcards

1
Q

Example of a ligand-gated ion channel

A

Nicotinic ACh receptor

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2
Q

Example of a G protein-coupled receptor

A

Muscarinic ACh receptor

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3
Q

Example of a kinase-linked receptor

A

Cytokine receptors

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4
Q

Example of a nuclear receptor

A

Oestrogen receptor

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5
Q

Nicotinic acetylcholine receptors

A
  • Permeable to Na+, K+, Ca2+
  • Nonspecific cation channel
  • Expressed on the post-ganglionic neuronal cell in ANS
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6
Q

Describe neurotransmission (events at the synapse)

A
  • Action potential travels down the presynaptic neuron —> calcium influx
  • NTs carried in vesicles until they fuse with the membrane of presynaptic neuron —> released into synapse
  • NTs bind to receptors on postsynaptic neuron until threshold is reached
  • Excitation, action potential
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7
Q

Drugs that act as agonists at Nicotinic ACh receptors

A

Acetylcholine (full)
Nicotine (full)
Varenicline (partial - good sub for nicotine withdrawal)

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8
Q

What binds and activates adrenoreceptors

A

Adrenaline and noradrenaline

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9
Q

Example of a G-protein coupled receptor

A

Adrenoceptors

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10
Q

MLCK

A

Responsible for smooth muscle contraction

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11
Q

Adrenaline binding to a1 adrenoceptor

A

Vasoconstriction
Gq - activation of phospholipase C

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12
Q

Adrenaline binding to a2-adrenoceptor

A

Relaxation of GI tract
Presynaptic inhibition of noradrenaline in CNS
Gi - inhibition of adenylyl cyclase

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13
Q

Adrenaline binding to B1-adrenoceptor

A

Increased HR and cardiac muscle contraction
Gs - stimulation of adenylyl cyclase, increased cAMP)

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14
Q

Adrenaline binding to B2-adrenoceptor

A

Bronchodilation
Increased HR and cardiac muscle contraction
Gs - stimulation of adenylyl cyclase, increased cAMP)

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15
Q

Adrenaline binding to B3-adrenoceptor

A

Thermogenesis in skeletal muscle, lipolysis
Gs - stimulation of adenylyl cyclase, increased cAMP)

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16
Q

Adrenaline

A

Binds to ALL adrenoceptors

Full sympathetic physiological response

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17
Q

Isoprenaline

A

Binds to B1 and B2 adrenoceptors

Tachycardia and bronchodilation

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18
Q

Salbutamol

A

Binds to B2 adrenoceptors

Bronchodilation
Treats acute symptoms of asthma

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19
Q

Theophylline

A

Phosphodiesterase inhibitor (terminates action of cAMP)

Indicated for COPD

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20
Q

Example of a kinase-linked/enzyme-coupled receptor agonist

A

Insulin

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21
Q

Signalling cascade effects activated by insulin receptor

A
  • Recruitment of glucose transporters
  • Increased formation of glycogen
  • Increased formation of fat
  • Changes in gene expression
  • Decreased glycogen to glucose conversion
  • Increased formation of protein
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22
Q

What are Nuclear receptors

A
  • Intracellular receptors (located in nucleus) bound by steroid hormones
  • Hormone-receptor complex binds to DNA and affects gene transcription
23
Q

What binds to nuclear receptors

A

Steroid hormones

24
Q

Steroid hormones are …. and pass through plasma membrane to bind to …

A

Hydrophobic/lipophilic

Nuclear receptors

25
Q

Receptor: androgen
Ligand:

A

Testosterone

26
Q

Receptor : oestrogen
Ligand:

A

17beta- oestradiol

27
Q

Receptor: glucocorticoid
Ligand:

A

Cortisol, corticosterone

28
Q

Receptor: progesterone mineralocorticoid
Ligand:

A

Progesterone

29
Q

Receptor: aldosterone receptor
Ligand:

A

Aldosterone

30
Q

Aldosterone is secreted in response to …

A

Hyponatremia (low Na+ in blood) - causes resistance to thiazides

31
Q

Thiazides

A

A type of diuretic — reduce fluid build-up in the body (lowers BP)

32
Q

Condition: hypokalaemia

A

Low K+ levels in blood

33
Q

Drug targets can be divided into 4 main categories:

A

Receptors
Enzymes
Ion channels
Carrier proteins

34
Q

What is ibuprofen

A

An anti-inflammatory drug

35
Q

Indication for ibuprofen

A

Pain and inflammation in rheumatic disease and musculoskeletal disorders

36
Q

Mechanism of action for ibuprofen

A

Decreases blood flow by inhibition of prostaglandins (usually causes vasodilation)

37
Q

Pharmacokinetics of ibuprofen

A

Half life = 1.2 - 2hrs
Liver disfunction = 3.1-3.4hrs

38
Q

Side effects of ibuprofen

A

Irritation of GI tract
Impairment of renal function

39
Q

What is amlodipine

A

Calcium channel blocker

40
Q

Indication of amlodipine

A

Angina and hypertension

41
Q

Pharmacokinetics of amlodipine

A

Long half life (40hrs)
Over 50hrs if renal disfunction

42
Q

Side effects of amlodipine

A

Reduction in arterial BP
Reduction in smooth muscle contraction

NOT SUITABLE FOR EMERGENCY

43
Q

What are selective serotonin re-uptake inhibitors (SSRIs) indicated for

A

Depression

Antagonist binds (blocks) serotonin receptors. More serotonin at synapse

44
Q

Symptoms of SSRIs

A

MANY

Anxiety, weight changes, headache, arrhythmias, constipation, nausea etc…

45
Q

Examples of SSRIs

A

Citalopram
Escitalopram
Fluoxetine
Fluvoxamine
Paroxetine
Sertraline

46
Q

Sodium valproate

A

Treats epilepsy and bipolar disorder

47
Q

Amitriptyline

A

(Tricyclic) Antidepressant

48
Q

Side effects of amitriptyline

A

Sedation (H1 receptor blockage)
Dry mouth and constipation (mACh receptor blockage)

49
Q

Pindolol

A

Treats hypertension

Partial agonist, Beta-blocker

Indicated for ventricular tachycardias, atrial fibrillation

50
Q

Isoprenaline and propranolol bind to …..

A

The same B1-adrenoceptor

51
Q

What does propranolol do

A
  • Blocks adrenaline
  • Activation of B1 results in reduction of HR and force of contraction
  • Can also bind to B2
52
Q

Why does propranolol cause pharmacodynamic drug interaction

A
  • Also has affinity for B2, blocks action of salbutamol
    —> exacerbate symptoms for asthmatic patients
    —> reduce effect of salbutamol
53
Q

Aspirin

A

Anti-platelet drug (blood thinner) - Prevents blood clotting

Also used as a painkiller

Irreversible competitive antagonist

Foundations Of Medicine 1 (3 decks)

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