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Medications > Medications pharmacodynamics and pharmacokinetics > Flashcards

Medications pharmacodynamics and pharmacokinetics Flashcards

1
Q

What are the contra indications of Haloperidol

A

CNS depression, history of ventricular arrhythmia, parkinsons disease, QT interval prolongation, recent myocardial infarction,

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2
Q

what are the main side effects of haloperidol

A

depression, eye disorders, nausea, neuromuscular dysfunction, weight decreased, arrhythmias, constipation, dry mouth, movement disorders, QT interval prolongation

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3
Q

what is the mechanism of action for haloperidol

A

antipsychotic that works by blocking post synaptic dopamine receptors particularly D2 receptors in the brain

antagonising effect
reduces dopamine activity which alleviates symptoms

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4
Q

how is the absorption of haloperidol

A

haloperidol is lipophilic and therefore readily absorbed

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5
Q

what is haloperidols peak plasma concentration with oral administration

A

1-6 hours

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6
Q

what is haloperidols bioavailability after first pass hepatic metabolism

A

40-75%

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7
Q

what is haloperidols peak plasma concentration with intramuscular administration

A

20 minutes

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8
Q

where is haloperidol metabolised

A

metabolised in the liver with only 1% of the administered dose excreted unchanged in urine

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9
Q

what is haloperidols half life

A

14.5-26 hours

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10
Q

what is the mechanism of action for lorazepam

A

binds onto post synaptic GABA receptors
this will cause an increase of GABA inhibitory effects on the central nervous system
= open up more chloride ion channels
= makes the neuron less responsive
= more relaxed and promote calming and sedating effect

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10
Q

what is the absorption of lorazepam and bioavailability

A

readily absorbed with bioavailability of 90% when given orally

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11
Q

what is peak plasma concentration of lorazepam

A

2 hours

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12
Q

how is lorazepam metabolised and how is it eliminated

A

hepatically metabolised and mainly eliminated by the kidneys with around 88% recovered in urine

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13
Q

what is lorazepam half life

A

14 hours

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14
Q

what is clozapines mechanism of action

A

antagonism of D2 Dopamine receptors and serotonin receptors
= reduces positive symptoms

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15
Q

how well is clozapine absorbed and peak plasma concentration time

A

almost complete absorption and peak plasma occuring between 1 to 6 hours

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16
Q

what is clozapines bioavailability like and why

A

low oral bioavailability because it primarily undergoes first pass metabolism in the liver

  • it is broken down before reaching the blood stream
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17
Q

what is clozapines metabolism like and excretion

A

almost completely metabolised and only a small amount of unchanged clozapine is detectef in the urine and faeces

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18
Q

what is clozapines half life

A

ranges from 4 to 12 hours

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19
Q

what is the mechanism of action of olanzapine

A

blocks dopamine D2 receptors antagonising effect = reduce positive symptoms
and also blocks serotonin receptors
= improve negative symptoms

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20
Q

absorption of olanzapine and peak plasma concentration

A

well absorbed after oral administration reaching peak plasma concentrations within 5-8 hours

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21
Q

what is olanzapines bioavailability

A

60%

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22
Q

metabolism of olanzapine and elimination

A

extensively metabolised in the liver and it is mainly eliminated through metabolism hence only 7% is found in its unchanged form

eliminated through 53% urine and 30% faeces

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23
Q

olanzapines half life

A

ranges between 21-54 hours
average 30 hours

24
Q

venlafaxine mechanism of action and pharmacodynamics

A

inhibits the reuptake of both serotonin and norepinephrine at the presynaptic terminal

this results in increased levels of neurotransmitters available at the synapse for post synaptic receptors to absorb

increased serotonin= associated with alleviation of depression symptoms

25
Q

venlafaxine absorption, peak plasma concentration and bioavailability

A

well absorbed with absolute bioavailability og 45%

peak plasma concentration 2-3 hours

26
Q

how is venlafaxine metabolised and what is the half life

A

metabolised mainly in the liver and eliminated via the kidneys through urine which is approx 87% of it being unchanged

half life approx 5 hours

27
Q

what is the mechanism of action and pharmacodynamics of sertraline

A

SSRI improves or relieves symptoms of depresion via the inhibition of serotonin reuptake at the pre synaptic neuron
= increased synaptic serotonin concentration

28
Q

absorption of sertraline
bioavailability and peak plasma concentration

A

slowly absorbed with peak concentrations occuring at 4-10 hours
bioavailability = 44%

29
Q

how is sertraline metabolised and excreted

A

heavily metabolised in the liver and because of that excretion of unchanged drug in urine is minor route

30
Q

half life of sertraline

A

approx 26 hours

31
Q

mechanism of action of salbutamol and pharmacodynamics

A

binds to beta 2 adrenergic receptors in the smooth muscle of the airways resulting in it relaxing = bronchodilation

= less airway resistance and more gas exchange

32
Q

salbutamol absorption and bioavailability

A

absorbed in the lungs on the bronchial smooth muscle
oral bioavailability is low

33
Q

how is salbutamol metabolised and eliminated and half life

A

metabolised in the liver and excreted in the urine with a half life of 2-5 hours

34
Q

Ipratropium bromide mechanism of action and pharmacodynamic

A

inhibit the action of acetylcholine on muscarinic receptors in the bronchial smooth muscle (antagonist)

muscarinic receptors mediate bronchoconstriction and mucus secretion therefore by blocking these receptors- ipatropium results in bronchodilation and decreased mucus production

= better airflow

35
Q

what is the absorption like for ipatropium bromide and peak plasma concentration and bioavailability

A

topically active but poorly absorbed
low peak concentrations after 1-2 hours
low bioavailability of 2%

36
Q

how is ipatropium bromide metabolised and how is it eliminated

A

metabolised in the gastrointestinal tract and about 90% of the dose is excreted unchanged via urine

37
Q

what is ipatropium bromides half life

A

1.6 hours

38
Q

what is the mechanism of action and pharmacodynamics of Carbocisteine

A

mucolytic agent works by modifying the structure of mucus making it less viscous and easier to expel
it breaks down the bonds in mucoproteins and restores fluidity of mucous
= easier to clear mucus which reduces airway obstruction and improves air flow

39
Q

what is the absorption like for Carbocisteine and peak plasma concentration

A

rapidly absorbed in the gastrointestinal tract with peak concentrations achieved within 1-2 hours

40
Q

where is Carbocisteine metabolised and eliminated

A

metabolised in the liver and around 36-60% of an administered dose is detected unchanged in the urine

41
Q

what is half life of carbicostine

A

1.3 hours

42
Q

Amoxicillin mechanism of action and pharmacodynamics

A

competitively inhibits penicillin binding proteins
it inhibits the bacterial cell wall synthesis therefore cell walls become weaker and stops the growth of bacteria

43
Q

what is the absorption like for Amoxicillin, bioavailability

A

well absorbed orally with a bioavailability of 60%

44
Q

Amoxicillin- how is it metabolised and what is the route of elimination

A

minimally metabolised in the liver and excreted primarily through the kidneys in the urine around 70-78% eliminated after 6 hours

45
Q

what is the half life of Amoxicillin

A

approx 1- 1.5 hours

46
Q

Prednisolone what are the mechanism of action and pharmacodynamics

A

corticosteroids bind to receptors inhibiting pro inflammatory signals

it exerts anti-inflammatory signals and immunosuppressive effects - decrease inflammation and immune response

inhibits activation of T cells

decrease vasodilation and permeability of capillaries therefore minimising tissue swelling

47
Q

what is the absorption like and bioavailability for Prednisolone

A

well absorbed orally with peak plasma concentration reached within 1-2 hours and 70% bioavailable

48
Q

Prednisolone metabolism and excretion

A

extensively metabolised in the liver and excreted mainly in the urine

49
Q

Mannitol - mechanism of action and pharmacodynamics

A

osmotic diuretic = increasing osmolarity therefore it reduces water reabsorption

water is drawn out of the cells which reduces fluid volume

promotes a osmotic water gradient promoting water movement = reduces intracranial pressure

49
Q

Prednisolone- half life

A

2-3 hours

50
Q

Mannitol- absorption

A

absorbed intravenously- high absorption

51
Q

Mannitol- metabolism and elimination

A

minimal metabolism in the body
excreted unchanged in the urine - approx 80% of the dose is eliminated within 3 hours of administration

52
Q

mannitol- half life

A

4.5 hours

53
Q

what is the mechanism of action of paracetamol and pharmacodynamic

A

inhibits an enzyme in the brain which results in decreased production of prostaglandins involved in pain
so paracetamol stops chemical messengers by reducing the pain signals to the brain

overall reduces pain by decreasing prostaglandin production

54
Q

paracetamol - pharmacokinetics absorption and peak plasma concentrations

A

rapidly absorbed in the gastrointestinal tract with peak plasma concentrations reached within 30-60 minutes and bioavailability of 88% bioavailability

55
Q

paracetamol- metabolism and elimination

A

mainly metabolised in the liver and mainly excreted in the urine
90% of the administered dose is excreted within 24 hours

56
Q

what is the half life of paracetamol

A

2-4 hours

57
Q
A

Medications (5 decks)

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