DRUG NAMES

Question 1

Vesamicol

Answer 1

ACh Vesicular transporter inhibitor

Question 2

Hemicholinium

Answer 2

Choline transporter inhibitor

Question 3

Varenicline

Answer 3

a4b2 partial agonist

Question 4

Haloperiodol

Answer 4

D2R antagonist

Question 5

Bromocriptine

Answer 5

D2R agonist

Question 6

Suxamethonium

Answer 6

Skeletal muscle relaxant via NMJ depol block

Question 7

Vercuronium

Answer 7

Skeletal muscle relaxant via NON- depol block

*competing for the cholinoceptors at the motor end plate thereby exerting its muscle-relaxing properties which are used adjunctively to general anesthesia

Question 8

Desipramine

Answer 8

Similar to cocaine - inhibits reuptake of NA. It is a tricyclic antidepressant (TCA).

Question 9

List a MAO-A Inhibitor and a MAO B isoform inhibitor

Answer 9

MAO-A Inhibitor - Moclobemide

MAO-B Inhibitor (DA selectivity) - Selegiline (used as adjunct with L-DOPA)

Question 10

List a COMT inhibitor. COMT inhibitors are used as adjunct therapy in ___

Answer 10

Entacapone. Parkinsons

Question 11

Carbidopa

Answer 11

inhibits DDC peripherally

Question 12

alpha methyl para tyrosine (AMPT)

Answer 12

Tyrosine hydroxylase inhibitor, Dopamanergic pathways can be excit or inhibit – Subset of motor disorders (some dystonias/dyskinesias) where there is overactivation of pathway SE: causes depression

Question 13

Dopamine is affected by MAO and COMT and Aldehyde dehydrogenase converts these affected intermediates into DOPAC (Dihydroxyphenyl acetic acid) or Homovanillic acid (HVA). It is where potential for reactive metabolities forming comes in. It can make dopamergic nerves more sensitive due to oxidative stress

Answer 13

Dopamine is affected by MAO and COMT and Aldehyde dehydrogenase converts these affected intermediates into DOPAC (Dihydroxyphenyl acetic acid) or Homovanillic acid (HVA). It is where potential for reactive metabolities forming comes in. It can make dopamergic nerves more sensitive due to oxidative stress

Question 14

List 5-HT2A agonists (3) and antagonists (2)

Answer 14

Ag (Hallucinogenics): LSD, DOI, psilocybin

Antag (Antipsychotics): Clozapine (best antipsychotic as it has affinity to lots of receptors and transporters), atypical antipsychotics

Question 15

List 5-HT2B agonists (3) and antag (1)

Answer 15

Ag: Fenfluramine (disrupting 5-HT vesicular storage of the neurotransmitter, and reversing serotonin transporter function) , Benflurorex, MDMA (ecstasy)
*Appetite suppressants BUT cause valvulopathies

Antag: Methysergide
*Migraine

Question 16

List 5-HT2C agonist and antagonist

Answer 16

Ag: Lorcaserin (anti-obesity. aids in treating addiction)

Antag: Agomelatine (depression, Generalized anxiety disorders (GAD) by increasing dopamine)
*As it is a melatonin receptor agonist - you have to take it before going to bed rather than in the morning

Question 17

?Ergotamine

Answer 17

5-HT2B antagonist?

• Furthermore, it is an antagonist at the 5-HT2C receptor, while at the 5-HT1A receptor it serves as a partial agonist
• Also binds to 5-HT2A receptor

Question 18

Spantide

Answer 18

Peptide NK1 R antag

Question 19

Aprepitant

Answer 19

Non-peptide NK1 R antag - used as an antimimetic AKA for the prevention of chemotherapy-induced nausea and vomiting

Question 20

Neprilysin

Answer 20

Metallopeptidase degrading Sub P

Question 21

Urocortin

Answer 21

CRF2 Agonist

Question 22

CRF

Answer 22

CRF1 Agonist

Question 23

Somatropin

Answer 23

Form of human growth hormone important for the growth of bones and muscles. Somatropin is used to treat growth failure in children and adults who lack natural growth hormone.

Question 24

Octreotide

Answer 24

Long-acting analogue of somatostatin - used to treat gigantism in children AND acromegaly in adults (an excess prod GH due to benign pituitary tumour)

Question 25

List 4 types of drugs that potentiate the GABA A receptor

Answer 25

1) Benzodiazepines – Diazepam, flumazenil
2) Barbituates – pentobarbitone
3) Neurosteroids – alphaxalone
4) Anticonvulsants – tiagabine, vigabatrin

Question 26

List 3 drugs that inhibit GABA A receptor

Answer 26

1) Bicuculline – decrease GABA binding
2) Picrotoxin – binds in pore, prevents Cl- flux
3) Penicillin – open channel blocker
* ALL these compounds, if in high enough doses = seizures

Question 27

List a drug that activates GABA A receptors

Answer 27

Muscimol aka magic mushroom (hyperpolarises) – hallucinogen

Question 28

GABA B agonist and antagonist

Answer 28

Ag: Baclofen – acts in spinal cord to reduce muscle spasm
Antag: Saclofen

Question 29

What blocks the action of Glycine? GABA?

Answer 29

Strychnine, Bicucullinae

Question 30

GAT-1 blocked by what drug? How does it work?

Answer 30

Tigabine (anticonvulsant, useful in PTSD, neuropathic pain, tonic spasms in MS)
-It decreases GABA uptake by neuronal and extraneuronal tissues

Question 31

Vigabatrin

Answer 31

Irreversible inhibitor of GABA transaminase. Potential to cause psychiatric disorders (depression and psychosis)

Question 32

Gabapentin

Answer 32

Developed as GABA analogue. Increases release of GABA by unknown mechanism

Question 33

NMDA channel blockers - list 2

Answer 33

Phencyclidine (PCP) and ketamine

Question 34

Glycine site antagonist

Answer 34

Kynurenate

Question 35

Polyamine site antagonist

Answer 35

Ifenprodil

Question 36

Riluzole

Answer 36

Anti-Glu used to treat ALS

* blocks TTX-sensitive sodium channels

Question 37

Memantine

Answer 37

Anti-parkinsonian, Inhibits NMDA receptor induced current

• Neuroprotection by low-affinity, uncompetitive, open-channel blockade of NMDA R
• Open channel blockade = spares normal neurotransmission
• Neuroprotective = decreases stroke damage
• Treats alzheimer’s disease, retinal degen/glaucoma, neuropathic pain, OCD

Question 38

Pindolol

Answer 38

Beta blocker/Partial 5HT1A/1B/1D autoR antag - blocks autoR so that 5-HT release is not inhibited