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
venlafaxine mechanism of action and pharmacodynamics
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
venlafaxine absorption, peak plasma concentration and bioavailability
well absorbed with absolute bioavailability og 45% peak plasma concentration 2-3 hours
26
how is venlafaxine metabolised and what is the half life
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
what is the mechanism of action and pharmacodynamics of sertraline
SSRI improves or relieves symptoms of depresion via the inhibition of serotonin reuptake at the pre synaptic neuron = increased synaptic serotonin concentration
28
absorption of sertraline bioavailability and peak plasma concentration
slowly absorbed with peak concentrations occuring at 4-10 hours bioavailability = 44%
29
how is sertraline metabolised and excreted
heavily metabolised in the liver and because of that excretion of unchanged drug in urine is minor route
30
half life of sertraline
approx 26 hours
31
mechanism of action of salbutamol and pharmacodynamics
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
salbutamol absorption and bioavailability
absorbed in the lungs on the bronchial smooth muscle oral bioavailability is low
33
how is salbutamol metabolised and eliminated and half life
metabolised in the liver and excreted in the urine with a half life of 2-5 hours
34
Ipratropium bromide mechanism of action and pharmacodynamic
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
what is the absorption like for ipatropium bromide and peak plasma concentration and bioavailability
topically active but poorly absorbed low peak concentrations after 1-2 hours low bioavailability of 2%
36
how is ipatropium bromide metabolised and how is it eliminated
metabolised in the gastrointestinal tract and about 90% of the dose is excreted unchanged via urine
37
what is ipatropium bromides half life
1.6 hours
38
what is the mechanism of action and pharmacodynamics of Carbocisteine
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
what is the absorption like for Carbocisteine and peak plasma concentration
rapidly absorbed in the gastrointestinal tract with peak concentrations achieved within 1-2 hours
40
where is Carbocisteine metabolised and eliminated
metabolised in the liver and around 36-60% of an administered dose is detected unchanged in the urine
41
what is half life of carbicostine
1.3 hours
42
Amoxicillin mechanism of action and pharmacodynamics
competitively inhibits penicillin binding proteins it inhibits the bacterial cell wall synthesis therefore cell walls become weaker and stops the growth of bacteria
43
what is the absorption like for Amoxicillin, bioavailability
well absorbed orally with a bioavailability of 60%
44
Amoxicillin- how is it metabolised and what is the route of elimination
minimally metabolised in the liver and excreted primarily through the kidneys in the urine around 70-78% eliminated after 6 hours
45
what is the half life of Amoxicillin
approx 1- 1.5 hours
46
Prednisolone what are the mechanism of action and pharmacodynamics
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
what is the absorption like and bioavailability for Prednisolone
well absorbed orally with peak plasma concentration reached within 1-2 hours and 70% bioavailable
48
Prednisolone metabolism and excretion
extensively metabolised in the liver and excreted mainly in the urine
49
Mannitol - mechanism of action and pharmacodynamics
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
Prednisolone- half life
2-3 hours
50
Mannitol- absorption
absorbed intravenously- high absorption
51
Mannitol- metabolism and elimination
minimal metabolism in the body excreted unchanged in the urine - approx 80% of the dose is eliminated within 3 hours of administration
52
mannitol- half life
4.5 hours
53
what is the mechanism of action of paracetamol and pharmacodynamic
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
paracetamol - pharmacokinetics absorption and peak plasma concentrations
rapidly absorbed in the gastrointestinal tract with peak plasma concentrations reached within 30-60 minutes and bioavailability of 88% bioavailability
55
paracetamol- metabolism and elimination
mainly metabolised in the liver and mainly excreted in the urine 90% of the administered dose is excreted within 24 hours
56
what is the half life of paracetamol
2-4 hours
57