Drugs part 2 Flashcards

1
Q

Structure of adrenoceptors

A

G protein coupled receptors

single polypeptide chain, 7 transmembrane alpha helices

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2
Q

alpha 1 adrenoceptor

A

binds to noradrenaline
Gq associated
alpha subunit dissociates and binds to phospholipase C
generates IP3 and DAG
IP3 binds to receptor on ER, causes calcium release
DAG activates PKC

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3
Q

Alpha 2 adrenoceptor

A

Gi protein (inhibitory)
alpha subunit inhibits to adenylyl cyclase
decreased PKA

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4
Q

beta 1,2 and 3 adrenoceptors

A

Noradrenaline
Gs protein
stimulates adenylyl cyclase
increased PKA

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5
Q

Where are beta 1 adrenoceptors found and what do they do?

A

Heart

increase heart rate, conduction velocity and increased contraction

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6
Q

What do beta 2 adrenoceptors cause?

A

dilation of blood vessls and bronchi

ciliary muscle relaxation

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7
Q

Which adrenoceptors cause blood vessel constriction?

A

Alpha 1 and 2

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8
Q

When can dobutamine be used as an adrenoceptor agonist?

A

beta 1 receptor agonist

heart failure, heart block

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9
Q

What are the differences between nicotinic and muscarinic AChRs?

A

Nicotinic receptors are ionotropic - acts as a channel for positively charged ions (sodium) to flow to cause depolarisation, all are excitatory
Muscarinic receptors are G protein coupled receptors, can be excitatory or inhibitory

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10
Q

M1 Muscarinic receptors

A

neural, including ganlia in stomach

IP3 pathway

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11
Q

M2 muscarinic receptors

A

cardiac

inhibits cAMP pathway

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12
Q

M3 muscarinic receptors

A

smooth muscle

increases IP3 stimulation

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13
Q

clinical uses of antimuscarinic drugs

A

asthma
bradycardia
to decrease gut motility
urinary incontinence

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14
Q

Drugs for GORD (supression of acid)

A

proton pump inhibitors (omeprazole)
H2 blockers - blockers histimine which stimulates acid secretion
Antacids increase pH
alginates form a physical barrier

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15
Q

What is helicobacter pylori and what can it cause?

A

gram negative bacteria
peptic ulcers disease - gastritis
hypergastrinaemia - increases gastrin release and decrease somatostatin release

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16
Q

What can be used to treat IBD?

A
aminosalicylcates 
immunomodulators 
corticosteroids
biologics 
- blocks TNF-a which is an inflammatory cytokine
17
Q

Types of laxatives

A

stimulant
osmotic
bulk

18
Q

Anti-diarrhoeals

A

loperamide
suppresses motility
allows more time for water to be absorbed

19
Q

What is suxamethonium apnoea?

A

occurs when this muscle relaxant has been given during surgery, patient can’t metabolise drug quickly enough, patient remains paralysed and unable to breathe after surgery

20
Q

What are the 4 categories of metabolising (and what do they metabolise)?

A
ultrarapid
extensive
intermediate
poor metabolisers
- cant metabolise CYP2D6
21
Q

What makes people high metabolisers?

A

High levels of CYP3A5

22
Q

What are examples of NSAIDs

A

aspirin
ibuprofen
paracetamol

23
Q

How do NSAIDs work?

A

Prevent the production of prostaglandins by inhibiting cyclooxygenase (COX)

24
Q

What are the 3 effects of NSAIDs?

A

analgesia - inability to feel pain
anti-inflammatory - PGs are involved in inflammation
anti-pyretic - reduce raised body temperature

25
Q

Which NSAID causes the irreversible inhibition of COX?

A

aspirin

26
Q

Which NSAID causes the reversible inhibition of COX?

A

ibuprofen

27
Q

Which NSAID causes the reversible non-competitive inhibition of COX?

A

paracetamol

28
Q

What is the difference between COX1 and COX2?

A

COX1 expressed by all cells

COX2 expressed by inflammatory cells

29
Q

Where are micerlocorticoids secreted from?

A

Outer zona glomerulosa

30
Q

Where are glucocorticoids secreted from?

A

middle zona fasciculata

31
Q

Where are adrenal androgens secreted from?

A

inner zona reticularis

32
Q

Mechanism of action of steroids

A

steroid receptors are inside the cell
when ligand engages with receptor they homodimerise
This causes translocation to the nucleus
Interacts with promoter regions on genes

33
Q

negative feedback of glucocorticoid release

A

Hypothalamus reduces corticotrophin releasing factor
This stimulates pituitary to release ACTH
ACTH finds adrenal cortex
Steroids released from cortex
Negative feedback by secreted steroids