Mechanisms & Dose Responses

Question 1

Name the endogenous ligands of opioids

Answer 1

Endorphins

Enkephalins

Question 2

Name some agonists of opioids

Answer 2

• Morphine
• Codeine
• Buprenorphine
• Heroin
• Fentanyl
• Methadone

Question 3

Name an antagonist of opioids

Answer 3

Naloxone

Question 4

Define endorphins

What are the opioid receptor subtypes

Answer 4

A family of endogenous opioid peptides

μ, δ, κ and NOP

Question 5

What sort of agonist is buprenorphine

Answer 5

Partial agonist

=> submaximal response

Question 6

MOA of opioid agonist drugs

Answer 6

Question 7

How are we trying to change the target for opioid drugs

Answer 7

We are trying to form a biased response to the G protein pathway only, to produce the analgesic effects and NOT affect the beta arrestin pathway (responsible for adverse effects)

Question 8

What is codeine a constituent of

Answer 8

The opium poppy (with morphine)

Question 9

How does codeine compare to morphine in terms of addictiveness

Answer 9

Codeine is much less potent than morphine making it less addictive

Question 10

MOA of naloxone

Answer 10

Question 11

What activates the beta receptor

Answer 11

Endogenous catecholamine NT (noradrenaline) released from nerve terminals

Adrenaline (epinephrine) can activate beta receptors following release from the adrenal gland

Question 12

How does adrenaline act as a drug

Answer 12

Question 13

What sort of drug is propranolol

Answer 13

A non selective beta receptor antagonist - blocks both beta 1 and beta 2

Question 14

What does salbutamol/albuterol do

Answer 14

It selectively targets the beta 2 receptor subtype, meaning that beta 1 receptors are not activated, which would produce CV effects

Question 15

What was originally used to treat respiratory conditions

Answer 15

Adrenaline - but it binds to beta 1 and beta 2, so it not only opens airways but activates CV system too to increase HR and BP

Question 16

Name 3 NSAIDs

Answer 16

Aspirin

Ibuprofen

Paracetamol

Question 17

What is different about paracetamol as a NSAID

Answer 17

Analgesic and antipyretic but limited anti-inflammatory effects

• thus sometimes not classified as a NSAID

Question 18

Pathway for prostaglandin synthesis

Answer 18

Question 19

How does aspirin interfere with prostaglandin synthesis

Answer 19

Inhibits the COX enzyme, thus an ANTI-PLATELET drug

Question 20

Pathway for cholesterol synthesis

Answer 20

Question 21

How do statins (e.g. atorvastatin) interfere with cholesterol synthesis

Answer 21

Atorvastatin is a HMG-CoA reductase inhibitor

Question 22

What is vitamin K involved in

Answer 22

The synthesis of clotting factors

Question 23

MOA of warfarin

Answer 23

A vitamin K antagonist that interferes in clotting factor synthesis

Question 24

What is dopamine closely related to

Answer 24

Adrenaline and noradrenaline

Question 25

MOA of cocaine

Answer 25

Question 26

MOA of amphetamine

Answer 26

dopamine releasing agent Inhibits dopamine reuptake enhanced dopamine effects

Question 27

MOA of methylphenidate (ritalin)

Answer 27

Dopamine reuptake blocker =\> increased attention Used to treat ADHD

Question 28

MOA of SSRIs (e.g. fluoxetine)

Answer 28

Inhibition of serotonin reuptake - selective

Question 29

MOA of MDMA

Answer 29

A serotonin releaser and reuptake inhibitor

Question 30

How do benzodiazepines work

Answer 30

Question 31

Name an example of a benzodiazepine

Answer 31

Diazepam Treats seizures, difficulty sleeping

Question 32

MOA of THC (cannabis)

Answer 32

A CB1 receptor agonist Inhibits postsynaptic neuronal activity

Question 33

Pathway for bacterial cell wall synthesis

Answer 33

Question 34

MOA of penicillin

Answer 34

Inhibits transpeptidase, preventing corss-linking occuring and weakens the cell wall of the bacteria

Question 35

Name the 3 histamine subtype receptors

Answer 35

H1 H2 H3

Question 36

Colloquial name for H1 antagonists

Answer 36

Anti-histamines

Question 37

What sort of drug is mepyramine

Answer 37

A H1 competitive receptor antagonist

Question 38

Effect of histamine on the body

Answer 38

Can reduce electrically-stimulated contraction

Question 39

MOA of ethanol

Answer 39

* Targets ion channels (both ligand gated and G protein coupled) - particularly GABA-A * Targets nicotinic and glutamate receptors * Downstream mechanisms are also believed to be affected by ethanol