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Psychopharmacology > Other pharmacology > Flashcards

Other pharmacology Flashcards

1
Q

Examples of 5-HT3 antagonists

A

*ondansetron
*granisetron

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2
Q

Common adverse effect of 5-HT3 antagonists

A

constipation

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3
Q

Most common use of 5-HT3 antagonists

A

Nausea and vomiting n chemotherapy

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4
Q

Where do 5-HT3 antagonist mainly work?

A

chemoreceptor trigger zone area of the medulla oblongata

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5
Q

Agomelatine works how?

A

It acts as an agonist at melatonin M1 and M2 receptors, increasing melatonin, and as an antagonist at 5HT2C receptors, leads to the release of dopamine and norepinephrine in the frontal cortex.

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6
Q

Does agomelatine affect serotonin levels

A

No

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7
Q

Antihistamines block what

A

the effects of histamine at either H1 or H2 receptors

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8
Q

Which are the H2 receptor blockers

A

Cimetidine
Ranitidine

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9
Q

Which are the H1 receptor blockers

A

Diphenhydramine
Cetirizine
Chlorpheniramine
Cyclizine
Hydroxyzine

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10
Q

Some first generation antihistamines have use in psychiatry such as what?

A

Promethazine

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11
Q

Contra indications to first generation antihistamines

A

Benign prostatic hyperplasia
Angle-closure glaucoma
Pyloric stenosis (in infants)

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12
Q

How do barbituates work?

A

facilitate GABAA action by increasing the duration of chloride channel opening

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13
Q

How do benzodiazepines work?

A

increase the frequency of chloride channels

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14
Q

How should benzodiazepines be withdrawn?

A

switch patients to the equivalent dose of diazepam
reduce dose of diazepam every 2-3 weeks in steps of 2 or 2.5 mg
time needed for withdrawal can vary from 4 weeks to a year or more

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15
Q

How are benzos divided?

A

into hypnotics (short half-life) and anxiolytics (long half-life).

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16
Q

Describe benzodiazepine pharmokinetics - how well do they bind to plasma protein, where metabolised and lipophilic or lipophobic

A

They show high plasma protein binding (95% for diazepam). They are mainly metabolised in the liver. They tend to be highly lipophilic and rapidly cross the blood brain barrier and placental barrier.

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17
Q

What is bioavailability?

A

the percentage of drug that is detected in the systemic circulation after its administration

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18
Q

Give examples of biogenic amines.

A

Catecholamines (adrenaline, noradrenaline, and dopamine)
Serotonin
Histamine

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19
Q

What is biotransformation?

A

a metabolic process that takes place mainly in the liver, in hepatocytes (but also in the kidneys, intestine, adipose, skin, and the lungs) and helps to facilitate the excretion of both exogenous and endogenous substances

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20
Q

What is biotransformation Phase 1?

A

Oxidation with cytochrome P450 (most common)
Reduction
Hydrolysis

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21
Q

What is biotransformation Phase 2?

A

Adding hydrophilic groups to the original molecule

The most common method is conjugation with glucuronic acid. (glucuronidation) but also can be by:
Methylation
Acetylation
Sulfation
Conjugation with glutathione
Conjugation with amino acids (glycine, taurine, and glutamic acid)

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22
Q

What is biotransformation phase 3?

A

A chemical substance can undergo further metabolism and excretion. It classifies into the following:

ATP-binding cassette (ABC)
Solute carrier (SLC) transporters

Phase III reactions refer to the active transport of the compound into urinary or hepatobiliary system to facilitate elimination.

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23
Q

What is tegretol

A

Carbamazepine

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24
Q

How does carbamazepine work?

A

binds to sodium channels increases their refractory period

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25
Q

When is carbamazepine contraindicated?

A

a history of bone marrow depression
combination with monoamine oxidase inhibitors (MAOIs)

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26
Q

What is an important warning with carbamazepine?

A

Serious dermatological reactions (toxic epidermal necrolysis (TEN: also known as Lyell’s syndrome) and Stevens Johnson syndrome - both rare)

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27
Q

What was CATIE?

A

Clinical Antipsychotic Trials of Intervention Effectiveness (CATIE) Study was a nationwide clinical trial that compared the effectiveness of older (first available in the 1950s) and newer (available since the 1990s) antipsychotic medications used to treat schizophrenia.

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28
Q

What was Phase 1 CATIE

A

Phase I compared old and new antipsychotics.

CATIE compared four of the newer medications to one another, and to an older medication. Participants in CATIE were followed for 18 months

29
Q

What was phase 2 CATIE?

A

Phase II sought to provide guidance on which antipsychotic to try next if the first failed (either due to ineffectiveness or intolerability).

30
Q

Risk factors for Charles Bonnet

A

Advanced age
Peripheral visual impairment
Social isolation
Sensory deprivation
Early cognitive impairment

31
Q

Prevalence of CBS in visually impaired people

A

thought to be between 11 and 15 percent

32
Q

What was the first drug used specifically for psychosis.

A

Chlorpromazine

33
Q

What is important side effect of chlorpromazine

A

photosensitivity reactions

34
Q

What does hepatic clearance involve?

A

conversion of the parent drug into a different chemical entity by the liver enzymes

35
Q

What does renal clearance involve?

A

emoval of the drug from the plasma into the urine.

36
Q

Describe zero order kinetic reactions and give 2 examples

A

the clearance of a drug is constant and is not related to the concentration of drug in the plasma, ethanol and phenytoin

37
Q

Describe first order reactions

A

Here the clearance is related to the concentration of the drug in the plasma.

38
Q

What is difference between half life in zero and first order reactions

A

In first order reactions this is constant.
In zero order reactions it gets progressively shorter.

39
Q

Steady state is usually achieved by how many half lives?

A

4.5

40
Q

Risk factors for paradoxical reaction to Benzos

A

Learning disability
Extremes of age (elderly or young)
History of aggression or poor impulse control
Benzodiazepine with short half life
High dose benzodiazepine
Intravenous administration of benzodiazepine

41
Q

What is a pharmokinetic drug interaction

A

take place when one drug interacts with another at the level of metabolism, absorption or excretion.

42
Q

What is pharmodynamic drug interaction

A

when one drug directly alters the effect of another.

43
Q

Examples of pharmokinetic interaction

A

Enzyme induction/ inhibition (interference with metabolism)
Changes in gastrointestinal tract motility and pH (interference with absorption)
Chelation
Competition for renal tubular transport (interference with excretion)
Changes in protein binding

44
Q

Examples of pharmodynamic drug interaction

A

Synergism
Antagonism
Interaction at receptors (e.g. allosteric modulation)

45
Q

Which drugs may be affected in terms of their stability eg by moisture/light in environment, and therefore not be suitable for compliance aids?

A

Sodium valproate
Zopiclone
Venlafaxine
Topiramate
Methylphenidate
Mirtazapine
Olanzapine
Amisulpride
Aripiprazole

46
Q

What is V Max?

A

maximum rate of the catalysed-reaction

47
Q

What is KM?

A

the concentration of substrate that leads to half-maximal velocity.

48
Q

What model is used to estimate V max and kM

A

Michaelis-Menten

49
Q

How does ethosuximide work?

A

blocks T-type calcium channels in thalamic neurons

50
Q

Drugs with little to no first pass effect?

A

lithium
pregabalin

51
Q

Name the phenomenon of drug metabolism whereby the concentration of a drug is greatly reduced before it reaches the systemic circulation.

A

first pass effect

52
Q

Where is most concentration of drug lost in first pass effect

A

liver and gut wall

53
Q

What scale is used for discontinuation syndrome/symptoms?

A

The DESS (Discontinuation-emergent signs and symptoms scale), a 43-item rating scale

54
Q

Which antiP is most likely to cause sedation?

A

clozapine

55
Q

Very common side effects of carbamazepine?

A

leucopenia

ataxia, dizziness, somnolence

vomiting, nausea

urticaria

fatigue

56
Q

Common side effects of carbamazepine?

A

hrombocytopenia, eosinophilia

Oedema, fluid retention, weight increase, hyponatraemia and blood osmolarity decreased due to an antidiuretic hormone (ADH)-like effect, leading in rare cases to water intoxication accompanied by lethargy, vomiting, headache, confusional state, neurological disorders

diplopia and accommodation disorders (e.g. blurred vision), headache

dry mouth

57
Q

Drugs which undergo significant first pass effect?

A

imipramine
fluphenazine
morphine
diazepam
buprenorphine

58
Q

How does flumazenil work

A

a selective GABAA receptor antagonist
through competitive interaction

59
Q

How is flumazenil administered

A

IV

60
Q

Half life flumazenil

A

1 hour

61
Q

Which drug is is used for the complete or partial reversal of the sedative effects caused by benzodiazepines.

A

flumazenil

62
Q

It takes about 5 half-lives for a drug to be roughly what percent eliminated

A

97%

63
Q

In which type of kinetics is there a fixed half life?

A

1st order
Zero order there is no fixed half life

64
Q

Which type of kinetics is is described as non-linear

A

zero order kinetics

65
Q

Recommended mood stabliser in hepatic impairment?

A

lithium

66
Q

Which antidepressants should be avoided in Hepatic impairment?

A

best avoid TCA and MAOI

67
Q

Which antiPs are recommended in hepatic impairment

A

Paliperidone (if depot required)
Amisulpride
Sulpiride

68
Q

Herpes simplex encephalitis typically affects where?

A

temporal lobes and inferior

69
Q
A

Psychopharmacology (19 decks)

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