Pharmacology 1A Flashcards
1
Q
Salbutamol
A
- Treats Asthma
- relaxes airways
- agonist of Gs coupled B2-adrenergic receptor
2
Q
Propanolol
A
- antagonist
- blocks Gs coupled Beta-adrenergic receptor
- stops effects of adrenaline on heart
3
Q
Types of GPCR
A
- Gs - activation adenylyl cyclase
- Gi (alpha) - inhibition adenylyl cyclase
- Gq - activation Phospholipase C
- Gi (Beta Gamma) - opening ion channels
4
Q
Atropine
A
- Blocks muscarinic coupled acetylcholine receptor
- blocks effects of Ach on heart, dilates pupils, inhibits secretion
- treat bradycardia
- eye drops to cause mydriasis and cycloplegia
5
Q
Cimetidine
A
- competitive antagonist of Gs coupled H2 receptor
- blocks acid secretion in stomach
6
Q
Ibuprofen
A
- Pain killer
- competitive reversible inhibitor of COX-1 and COX-2 (which are involved in synthesis of prostanoids that induce inflammation)
7
Q
Aspirin
A
- anti-thrombotic drug
- irreversible covalent inactivation of COX-1 and COX-2 by acetylation of enzyme
- COX1 is involved in synthesis of platelets
- COX2 synthesises prostanoids
8
Q
Digoxin
A
- treats cardiac insufficiency
- Blocks Na/K ATPase
- Increase in intracellular Na
- Decrease in electrochemical gradient Na
- Decrease in Ca extrusion from cell
- More Ca in cell
- Increased contraction
9
Q
Buprenorphine
A
- partial agonist at mu-opioid receptor
- mu-opioids are good analgesics but have severe side effects
- used to treat pain and addiction
- high affinity but low efficacy
- less side effects
10
Q
Haloperidol
A
- antipsychotic
- dopamine receptor
11
Q
D-tubocurarine
A
- nictonic Ach receptor
- neuromuscular block
- muscle relaxation
- blocks postsynaptic ionotropic receptors
12
Q
Certolizumab pegol
A
- targets arthiritis
13
Q
Lignocaine
A
- local anaesthetic for pain relief
- blocks voltage-gated Na channels
14
Q
Phenytoin
A
- treats epilepsy
- blocks voltage-gated Na channels
15
Q
Tetrodotoxin
A
- toxicology
- experimental drug
- blocks voltage-gated Na channels
16
Q
Ziconotide
A
- neuropathic pain treatment
- blocks voltage-gated Ca channels
17
Q
Botulinum toxin A (Botox)
A
- blocks exocytosis of neurotransmitters
- balancing muscle tone in cerebral palsy
- treatment of hypersecretory disorders
18
Q
L-DOPA
A
- Treatment of Parkinsonism
- precursor of dopamine stimulates production
19
Q
Fluoxetine
A
- treatment of depression
- blocks presynaptic transmitter uptake
- prolongs transmitter action
20
Q
Neostigmine
A
- treatment of myasthenia gravis
- blocks transmitter breakdown
- prolongs transmitter actions
21
Q
Valium
A
- positive allosteric modulator of postsynaptic ionotropic receptor
- enhances transmitter effects
22
Q
M2 muscarinic receptors
A
- in the heart
- Gi/o -protein coupled
- decrease cAMP and Ca signalling
- decrease electrical excitability
23
Q
M3 (and M1) muscarinic receptors
A
- GI tract, airways, bladder, eye
- Gq- protein coupled
- Increased Ca signalling
- Contract smooth muscle
- stimulate glandular secretion
24
Q
α1 adrenergic receptors
A
- blood vessels, smooth muscles, eyes
- Gq-protein-coupled
- Increased Ca signalling
- Smooth muscle contraction
25
β1 adrenergic receptors
- Heart
- Gs-protein coupled
- Increased cAMP signalling
- Increased electrical excitability and muscle contractility
26
β2 Adrenergic receptors
- bronchi, uterus, GI tract, blood vessels (skeletal muscle and some others), liver, adipose tissue, bladder, eye
- Gs-protein-coupled
- Increased cAMP signallling
- relaxation of smooth muscle
- increased blood glucose concentration
27
Adrenaline
- used in cardiac arrest
- β1 agonist
28
Isoprenaline
- non-selective β agonist
- treatment of shock (now rarely used)
29
Dobutamine, dopamine
- β1 selective agonists
- used in cardiac arrest, cardiogenic shock, cardiac surgery
30
Atenolol
- β1 antagonist
- beta blockers
- treat CV disease
- treat anxiety
31
Glyceryl Trinitrate
- NO donor
- lowers blood pressure to treat angina
- rapid onset
32
Noradrenaline
- activates α1 receptors in vascular smooth muscle in skin, GI tract, kidneys - constriction.
- activates β2 receptors in vascular smooth muscle in heart, brain, lungs, skeletal muscle - relaxation
33
Phenylephrine
- α1 selective agonist
- treat acute hypotension
- OTC nasal decongestant
- side effects: hypertension and reflex bradycardia
34
Phentolamine
- reversible competitive α-antagonist
- control of hypertensions in phaeochromocytoma (tumour of the adrenal)
35
Prazosin
- α1 antagonist
- antihypertensive
- side effects: postural hypotension, headache, reflex tachycardia
- increase in urinary flow in benign postatic hyperplasia
36
Ipratropium
- M3 muscarinic receptor blocker
- muscle relaxation in asthma bronchiale
37
Salmeterol
- β2 selective agonist
- anti-asthmatic
- longer term action than salbutamol
38
Bethanechol
- stimulates GI motility
39
Pilocarpine
- increase saliva production
- lower raised intraocular pressure in glaucoma
40
Atropine/Hyoscine
- anti-spasmodic (IBS)
- reduce secretions as premedication for anaesthesia
- control ANS effects of blockers of ACh esterase
41
Pirenzepine
- reduce acid secretion in stomach - treatment for peptic ulcer (now rarely used)
42
Clenbuterol
- weight loss drug
- anabolic action
43
Darifenacin
- treatment of urinary frequency, urgency and incontinence
44
Tropicamide
- eye drops to cause mydriasis and cycloplegia
45
Timolol
- non-selective β antagonist
- eye drops for treatment of glaucoma
46
Glycopyrronium
- non-selective muscarinic antagonist
- reduce excessive perspiration
47
