Pharmacology Flashcards

1
Q

Components of pain

A
Affective
Cognitive
Discriminative
Arousal
Motor
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2
Q

Pain transmission horns

A

Non-noxious stimuli (dynamic allodynia) through A beta - Laminae 3 4 5 deep horns

Nociceptive mechanical and thermoceptive stimuli (polymodal, static allodynia) through A delta - Laminae 1 2o 5 superficial horns and some deep

Nociceptive mechanical, thermoceptive, and chemical stimuli (polymodal) through C - Laminae 1 2o superficial horns

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3
Q

Wide dynamic range horn

A

Horn 5

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4
Q

Serotonin excitatory and inhibitory receptors

A

5-HT1 = inhibitory

5-HT3 = excitatory

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5
Q

AMPA

A

More selective to sodium entry than calcium and the antagonist is CNQX (cyan quaxaline)

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6
Q

NMDA

A

repeated depolarisation is needed as well as two ligands (glu + gly), and the antagonists are ketamine (also used to treat depression) and memantine but neither are used any more clinically due to serious side-effects such as hallucinations and motor effects

There are presynaptic receptors but less studies on them, all we know is that the repeated depolarisation mechanism for releasing magnesium is not important for them

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7
Q

SP and NK-1

A

SP: co-released with NKA, CGRP, and glutamate

IP3: GPCR, postsynaptic, increases release of calcium from intracellular stores by generating IP3, antagonists have failed, involved in mood, stress, anxiety, and pain

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8
Q

Descending controls transmitter systems

A

Opioidergic, noradrenergic, and serotonergic

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9
Q

Morphine microinjection provides analgesia in which section?

A

PAG

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10
Q

What drugs cause schizophrenic attacks and susceptible patients?

A

LSD and phencyclidine

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11
Q

What receptor causes the psychedelic effects of LSD?

A

5HT2A

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12
Q

Which receptors does LSD not affect?

A

5HT3 5HT4

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13
Q

How does the immune system promote addiction?

A

TLR4

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14
Q

Tinazidine Contraindications

A

Should not be taken with fluvoxamine (antidepressant) or ciprofloxacin (antibiotic) either. If it is taken in high doses for a long time, it causes withdrawal effects.

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15
Q

Local Anaesthetic Nerve Fibre Order Of Action

A

L.As block in the following order: small myelinated axons (Ad), then unmyelinated axons (C- fibres), then large myelinated axons (Ab) & motor axons.

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16
Q

What does PABA inhibit?

A

Sulphonamide

17
Q

Drug-induced PD

A

Drugs that reduce the amount of dopamine in the
brain (e.g. reserpine).

Drugs that block dopamine receptors (e.g.
antipsychotics such as chlorpromazine).

18
Q

Which anti-epileptic drugs are highly bound to plasma proteins?

A

phenytoin & valproic acid

19
Q

What is the status of activity of antiepileptic drug metabolites?

A

they are active and also cleared through hepatic pathways, some of the older anti-epileptics are hepatic microsomal enzyme potentiators

20
Q

Valproate special use

A

In adolescents where grand & petit mal co-exist since it is effective against both (unlike most antiepileptics)

21
Q

Which drug is the first choice in absence seizures?

A

Ethosuximide (T subtype inhibited as it is the one responsible for absence seizures)

22
Q

Tiagabine and vigabatrin MOA

A

Tiagabine GAT1 inhibited reuptake

Vigabatrin GABA-T inhibited transaminase inactivation

23
Q

Uses of vigabatrin

A

Adjunct therapy in refractory complex partial seizures

West’s syndrome (infantile spasms)

24
Q

Which BZD is also an anti-depressant?

A

Alprazolam

25
Q

What is midazolam also used for?

A

Anaesthesia

26
Q

Which hypnotic reduces REM sleep the least?

A

Zolpidem (and BZDs relatively less), GH release is unaffected, SW reduced

27
Q

BZD duration of action

A

Diazepam: long acting for anxiolysis
Flurazepam: long acting for hypnosis
Temazepam: intermediate acting for hypnosis
Triazolam - short acting

28
Q

Which BZD has an active metabolite?

A

Nordazepam -> N-desmethyldiazepam (60 hour half-life)

29
Q

What is special about buspirone?

A

Takes long time to work (cannot be given for acute attack) and can be withdrawn abruptly and safely

30
Q

3Zs side effects

A

Zolpidem & zaleplon: nightmares, agitation, headache, G.I upset, dizziness

Zopiclone: taste alteration, impairment of driving skills, palpitations (following withdrawal from drug after prolonged use)

Zolpidem & zopiclone: anterograde amnesia
(more so than zaleplon)

31
Q

Which hypnotic causes endocrine changes and what are they?

A

Ramelteon, increase in prolactin and decrease in testosterone

32
Q

What is the danger in using tacrine?

A

Tacrine causes hepatotoxicity (liver damage/failure) too. Thus, it is required simultaneous monitoring for hepatotoxicity, recently not used much.

33
Q

Which AChE and BuChE inhibitor affects the heart?

A

Galantamine (also nAChRs enhancer)

Do not forget that memantine can also cause hypertension is a side-effect

34
Q

Which drug, if given in gradual doses, does not show as much side-effects?

A

Rivastigmine

35
Q

Which drug is given in gradual doses to avoid toxicity?

A

Carabamezepine

36
Q

Other Treatments For AD

A

Levetiracetam: An anticonvulsant with a novel mechanism of action (which is not clear), anti-inflammatory processes in the brain, may slowdown the AD progression.

Caprylidene (Caprylic triglyceride): A formulation of coconut oil, which release ketones, provide alternative energy source to glucose. It might be useful in mild to moderate AD to improve memory and cognitive function, but it does not reverse neuronal degeneration.

Curcumin (Extract of turmeric): It has both the anti-inflammatory and anti-oxidant properties that can suppress the formation of NFTS and Aβ deposit.

Latrepirdine (Dimebon): It is a weak inhibitor of AChE, BuChE, and NMDA receptors.

Methylthioninium chloride compound (MTC): It is a tau kinase inhibitor that reduce the formation of NFTs.

37
Q

Partition Co-efficient

A

(P = [organic]/[aqueous]).

38
Q

Examples of pharmacological approaches to bypassing the blood brain barrier

A

Chemical delivery system (lipidisation): enhanced delivery of ganciclovir to the bran by covalently attaching with 1-methyl-1,4-dihydronicotinate to a hydroxymethyl group.

Prodrug: Valacyclovir is a prodrug of acyclovir. In oral administration it rapidly gets converted to acyclovir.

Polymeric micelles: Pluronic P85 micelles loaded with a neuroleptic drug is targeted to the brain by conjugating micelles with neurospecific antibodies as targeting moieties.

Nanoparticles (ApoE-albumin): hexapeptide dalargin

39
Q

Why are CGRP antagonists not used?

A

Hepatotoxic