Pharmacopeia

Question 1

Thiazide diuretics

Answer 1

• Hypertension

Question 2

Naltrexone

Answer 2

• Agonist at the μ-opioid receptor antagonist
• Use:
  
  • Pre-clinical studies:
    
    • Alcohol addiction
    • Opiate addiction

Question 2

ACE inhibitors

Answer 2

• Inhibits angiotensin converting enzyme, thus decreasing reabsorption in the kidney
• Use:
  
  • Hypertension

Question 3

Formoterol

Answer 3

• A LABA - aka long acting B₂-ADR agonist
• ie a sympathomimetic, selective for B₂ adrenoceptors
• Used for:
  
  • Asthma
  • COPD

Question 4

Terbutaline

Answer 4

• SABA
• Use:
  
  • Asthma
  • COPD

Question 5

Salbutamol

Answer 5

• SABA
• Use: asthma

Question 6

Bupropion

Answer 6

• MOA still not fully known, but described as:
• Weak norepinephrine-dopamine reuptake inhibitor
• Use:
  
  • Nicotine addiction

Question 6

Disulfiram

Answer 6

• Acetaldehyde dehydrogenase inhibitor
• Use
  
  • Alcohol addiction
  • Stimulant addiction

Question 7

Ketamine

Answer 7

• NMDA receptor inhibitor

Question 8

Rimonabant

Answer 8

• Antagonist at the CB receptor
• Use:
  
  • Cannabis addiction
  • Obesity
  • Psychosis

Question 9

Fluoxetine

Answer 9

• aka Prozac
• an SSRI
• Use:
  
  • Depression
  • Stimulant addiction

Question 10

General anaesthetic

Answer 10

• MOA ?
• Removes cognition, and there can be no perception of pain without cognition

Question 10

Benzodiazepines

Answer 10

• MOA:
  
  • Enhance GABA activity
• Uses:
  
  • Depression
  • Alcohol addiction
  • Cocaine addiction

Question 10

Methoxsalen

Answer 10

• Slows metabolism of nicotine
• Reduces number of cigarettes smoked, as each has a longer lasting effect

Question 10

Naloxone

Answer 10

• μ-opioid receptor antagonist
• Use:
  
  • Opiate overdose

Question 12

Deep brain stimulation

Answer 12

• Activates the PAG, thus activating the descending pathway of analgesia

Question 13

Fenofibrates

Answer 13

• Use: dyslipidaemia
• MOA:
  
  • Decreases LDL, VLDL and TAGs
  • Increases HDL
  • By increasing catabolism of TAG-rich particles

Question 14

Statins

Answer 14

• eg Lipitor
• MOA: inhibit the enzyme that is needed for endogenous synthesis of cholesterol
• Use: hypercholesterolaemia

Question 15

Methadone

Answer 15

• Opiate replacement therapy
• Agonist at the opioid receptor

Question 16

Corticosteroids

Answer 16

• e.g. Prednisolone
• Immunosuppressive and anti-inflammatory
• Used for:
  
  • Asthma (inhaled, aka ‘preventer’)
  • COPD, not as useful as for asthma, but still used

Question 17

Ziconotide

Answer 17

• An omega conotoxin from Conus magus
• Inhibits N-type Ca_v channels in the spinal cord, inhibiting release of excitatory neurotransmitters from primary nociceptors
• Thus, prevents pain transmission
• Use:
  
  • Neuropathic pain

Question 18

Salmeterol

Answer 18

• LABA
• Use: asthma

Question 18

Clonidine

Answer 18

• α₂-adrenoceptor agonist
• Use
  
  • Analgesia
  • Hypertension
  • Clinical trials:
    
    • Opioid withdrawal

Question 20

Local anaesthetic

Answer 20

• eg Lignocaine
• Inhibits Na_v channels, thus inhibiting action potentials along the primary nociceptor afferents

Question 22

Codeine

Answer 22

• Weak agonist at the μ opioid receptor
• Use:
  
  • Pain

Question 23

Topiramate

Answer 23

• Use:
  
  • Epilepsy
  • Weight loss
  • Stimulant addiction
  • Depression

Question 24

Gabapentinoids

Answer 24

• eg **Pregabalin, **marketed as Prialt
• Modulator of Ca_v channels, decreases a influx into pre-synaptic terminals, thus decreasing neurotransmitter release from primary nociceptors
• Use:
  
  • Neuropathic pain

Question 26

NSAIDs

Answer 26

• eg Aspirin, ibuprofen
• Inhibits COX2, and thus prevents the production of prostaglandins etc.
• Decreases inflammatory noxious stimulus in the tissue
• Can also act on the PAG to stimulate the descending analgesic pathway

Question 28

Sativex

Answer 28

• THC + CBD
• MOA: agonist at the CB receptors
  
  • Pre-synaptically: inhibit Ca_v channels
  • Post-synaptically: hyperpolarisation of nociceptor projection neuron
  • RVM: activation of descending analgesic pathway
  • ? enhance anti-inflammatory action of glia in CNS
• Use:
  
  • Chronic pain: (AIDS, cancer related)
  • Spasticity (MS)
  • Anti-emetic and appetite stimulant (cancer)

Question 29

Metformin

Answer 29

• Suppresses glucose production in the liver
• Use:
  
  • Diabetes

Question 30

TCAs

Answer 30

• Tricyclic antidepressants, eg Amitryptilline
• Inhibit reuptake of NA and 5-HT at the synapse in the dorsal horn, thus prolonging the action of these neurotransmitters
• Results in inhibition of pain transmission

Question 32

Nadolol

Answer 32

• β₂-ADR inverse agonist
• Use:
  
  • Has been used experimentally in mice to show the role of empty β₂-ADRs in pathogenesis of asthma
  • Some early clinical data has shown that it can reduce the reactivity of airways

Question 33

Beta blockers

Answer 33

• Antagonists at the B₁-ADR in cardiac muscle
• Use: hypertension

Question 34

Varenicline

Answer 34

• nAChR partial agonist
• Used for:
  
  • Nicotine addiction

Question 35

Phentermine

Answer 35

• An anticonvulsant
• Use:
  
  • Epilepsy
  • Weight loss

Question 36

Morphine

Answer 36

• Agonist at the μ opioid receptor
• μ opioid receptors act in various locations to bring about analgesia:
  
  • Presynaptically: inhibit Ca_v channels
  • Post-synaptically: hyperpolarisation through activation of K+ channels
  • PAG: activation of descending analgesic pathway
• Use:
  
  • Analgesia

Question 37

Buprenorphine

Answer 37

• Partial agonist at the μ opioid receptor
• Use:
  
  • Opioid replacement therapy

Question 38

Baclofen

Answer 38

• MOA
  
  • Agonist at GABA receptors
  • Counters glutamate activity
• Use:
  
  • Spasticity
  • Clinical trials:
    
    • Alcohol addiction
    • Cocaine addiction