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year 3 > OSCE > Flashcards

OSCE Flashcards

1
Q

what is the mechanism of action amiodarone

A

Target: non-selective for Na channel, Ca channel and α-adrenoceptors
Action: Non-selective inhibitor of the above channels and receptor Effect: prolongs the cardiac action potential seen as an increase in the QT interval on the ECG
Overall effect: Class III antiarrhythmic effect

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2
Q

what are the side effects of amiodarone

A

Common side effects: Corneal microdeposits
Important:
Thyoid disorders – hypothyroidism, hyperthyroidism
Pulmonary fibrosis
Phototoxicity
Peripheral neuropathy
Optic neuritis/neuropathy (can lead to blindness)
Hepatotoxicity
Slate-grey skin discolouration

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3
Q

what are the interactions of amiodarone

A

Other anti-arrhythmic (increased myocardial depression)
Digoxin (amiodarone increases plasma digoxin concentration – halve digoxin dose)
Warfarin (increased anticoagulant effect)
Beta blockers, calcium channel blockers (increased risk of bradycardia, AV block and myocardial depression)
Simvastatin (increased risk of myopathy)
Tricyclic antidepressants (increased risk of ventricular arrhythmias)
Phenytoin (increased plasma phenytoin concentration)
Lithium (increased risk of ventricular arrhythmias)

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4
Q

what is the therapeutic indication of amiodarone

A

Starting dose – 200mg 3 times daily for 1 week then twice daily for the following week Maintenance dose – 200mg once daily

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5
Q

what formulations does amiodarone come in

A

Tablet, injection, solution

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6
Q

how is amiodrone metabolised

A

This drug is metabolized to the main metabolite desethylamiodarone (DEA) by the CYP3A4 and CYP2C8 enzymes.
Metabolised in the liver

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7
Q

how is amiodarone excreted

A

Via the liver and bile

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8
Q

what are the contraindications of amiodarone

A

Caution in heart failure and the elderly
Avoid in sinus bradycardia, sino-atrial heart block, thyroid dysfunction and iodine sensitivity
Avoid intravenous amiodarone in severe respiratory failure, circulatory collapse and severe arterial hypotension
Discontinue if patient develops optic neuritis/neuropathy

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9
Q

what are brand names for amiodarone

A

Cordarone, Nexterone

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10
Q

what is the absorption of amiodarone

A

The bioavailability is between 35-65%

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11
Q

what is the MoA of Amitriptyline

A

Target: Noradrenaline and serotonin reuptake transporters on the pre-synaptic neuronal membrane
Action: Inhibitor
Effect: Prevent re-uptake and subsequent degradation of the monoamine neurotransmitters serotonin and noradrenaline from the synaptic cleft
Overall effect: Prolonged presence of serotonin and noradrenaline in the synaptic cleft leads to prolonged neuronal activity – in mood disorders such as depression there are low levels of these neurotransmitters in the brain. TCAs therefore restore the concentration to normal levels.

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12
Q

what is the absorption of Amitriptyline-

A

The bioavailability is between 30-60%

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13
Q

what is the distribution of amitriptyline

A

Widely distributed around the body. The protein binding is around 95%

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14
Q

how is amitriptyline metabolised

A

Metabolised in the liver and CYP2D6, CYP2C19, CYP3A4

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15
Q

how is amitriptyline excreted

A

Excreted as urine around 12-80%

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16
Q

what formulations does amitriptyline come in

A

Tablets, solutions, capsule

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17
Q

what is the therapeutic indication for amitriptyline

A

Starting dose – 75mg daily (30-75mg if elderly) (lower doses for indications other than depression)in divided doses or as a single dose nocte
Maintenance dose – varies depending on drug; for amitriptyline 150-200mg

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18
Q

what are the side effects for amitriptyline

A

Antimuscarinic effects – dry mouth, blurred vision, constipation, urinary retention
CNS side effects (particularly in elderly) e.g. anxiety, dizziness, agitation, confusion
Weight gain
Important:
**Cardiotoxic in overdose – caution in patients at risk of suicide
Neuroleptic malignant syndrome
Hyponatraemia (particularly in elderly)

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19
Q

what are the interactions for amitriptyline

A

**MAOIs (risk of hypertensive crisis and hyperthermia) – do not start a tricyclic until 2 weeks after stopping an MAOI and vice versa, do not co-prescribe
Antiepileptics (seizure threshold lowered)
Alcohol (increased sedative effect)
Anti-arrhythmics (increased risk of ventricular arrhythmias)

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20
Q

what are the contraindications for Amitriptyline

A

Caution in cardiovascular disease, hepatic impairment (avoid if severe), hyperthyroidism, epilepsy, diabetes, prostatic hypertrophy, chronic constipation, urinary retention, glaucoma, the elderly and those at high risk of falls and of suicide
Avoid following MI, in heart block and in the manic phase of bipolar disorder
Discontinue if patient enters a manic phase

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21
Q

what is the brand name for amitriptyline

A

Elavil

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22
Q

what is the MoA of Azathioprine

A

Azathioprine is metabolised to the 6- mercaptopurine, which is then converted intracellularly to purine analogues. These purine analogues are incorporated into DNA and inhibit clonal expansion of B lymphocytes during the induction phase of the immune response. This results in suppression of the antibody-mediated response.

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23
Q

what is the absorption of Azathioprine

A

The bioavailability is 60%

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24
Q

what is the distribution of Azathioprine

A

Protein binding is between 20-30%

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25
Q

how is Azathioprine metabolised

A

Activated non-enzymatically, deactivated mainly by xanthine oxidase

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26
Q

how is Azathioprine excreted

A

Kidney; 98% as metabolites

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27
Q

what formulations does Azathioprine come in

A

tablets

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28
Q

what are the side effects of Azathioprine

A

Nausea
Cancer risk – azathioprine increases the risk of lymphoma and skin malignancies
Bone marrow suppression – anaemia, leucopenia, thrombocytopenia
Hypersensitivity reactions including interstitial nephritis – discontinue immediately
Pancreatitis

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29
Q

what are the interactions of Azathioprine

A

Allopurinol (risk of severe myelosuppression – do not co-prescribe) Warfarin (reduced anticoagulant effect) – may need to increase warfarin dose
Aminosalicylates (bone marrow toxicity – may require increased monitoring
Trimethoprim/co-trimoxazole (risk of blood disorders)

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30
Q

what are the contraindication of Azathioprine

A

Caution in hepatic and renal impairment
Avoid in patients with known hypersensitivity to mercaptopurine, those with thiopurine methyltransferase (TPMT) deficiency and in breastfeeding women

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31
Q

name the brand names of Azathioprine

A

Azasan, Imuran

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32
Q

what is the MoA of buprenorphine

A

Target: G-protein coupled opioid ‘mu’ receptors in the CNS and peripheral nervous system
Action: Full agonist (high affinity for receptors)
Effect: Closure of N-type voltage-dependent calcium channels and opening of calcium-dependent inwardly rectifying potassium channels – this increases potassium conductance. Opioids also presynaptically inhibit the release of pain-signalling neurotransmitters such as substance P.
Overall effect: Membrane hyperpolarisation and reduced neuronal excitability, reduction or inhibition of pain neurotransmission.

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33
Q

what is the absorption of buprenorphine

A

The bioavailability is Sublingual: 30%
Intranasal: 48%
Buccal: 65%

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34
Q

what is the distribution of buprenorphine

A

Protein binding is 96%

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35
Q

how is buprenorphine metabolised

A

liver

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36
Q

how is buprenorphine excreted

A

Via the bile duct and kidney

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37
Q

what are the formulation of buprenorphine

A

Plaster, film

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38
Q

what is the therapeutic indication for buprenorphine

A

For sublingual:
Adults: 200–400 micrograms every 6–8 hours.
For intravenous
Adults: 300–600 micrograms every 6–8 hours.

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39
Q

what are the side effects of buprenorphine

A 
Nausea/vomiting 
Constipation Important: 
Respiratory depression 
Hypotension 
Sedation and coma 
Tolerance 
Physical and psychological dependence 
Overdose – this is reversed with naloxone
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40
Q

what are the interactions of buprenorphine

A

CNS depressants (increased risk of respiratory depression) – alcohol, sedatives, hypnotics, general anaesthetics
MAOIs (potentiate action of morphine)
Alcohol (increased hypotensive and sedative effects)

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41
Q

what are the contraindications of buprenorphine

A

Caution in the elderly, hypotension, shock, prostatic hypertrophy, obstructive ir inflammatory bowel disorders, biliary disease, convulsive disorders, adrenocortical insufficiency, hepatic or renal impairment, pregnancy and patients with a history of drug dependence
Avoid in acute respiratory depression, coma, head injury or raised ICP (opioids interfere with pupillary responses used in neurological assessment) and those at risk of paralytic ileus

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42
Q

name the brand names of buprenorphine

A

Belbuca, Bunavail, Buprenex, Buprenorphine, Butrans, Probuphine, Sublocade, Suboxone, Subutex, Zubsolv

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43
Q

MoA of Carbamazepine

A
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44
Q

absorption of Carbamazepine

A

The bioavailability is between 75-85%

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45
Q

distribution of Carbamazepine

A

The protein distribution is between 70-80%

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46
Q

how is Carbamazepine metabolised

A

Hepatic- by CYP3A4

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47
Q

how is Carbamazepine excreted

A

Urine (72%)

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48
Q

list the different formulations of Carbamazepine

A

Tablets, capsule, suspension

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49
Q

what is the therapeutic indication of Carbamazepine

A

Starting dose – 100-200mg 1-2 times daily (reduce if elderly); Maintenance dose 0.8-1.2g daily

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50
Q

what is the adverse effects of Carbamazepine

A

Drowsiness
Nausea/vomiting
Ataxia, dizziness
Hyponatraemia (syndrome of inappropriate ADH secretion (SIADH))
Cardiac condution disturbances
Leucopenia/bone marrow failure
Stevens-Johnson syndrome (especially if Han Chinese or Thai origin due to HLA-B*1502 allele)

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51
Q

what are the interactions of Carbamazepine

A

Warfarin (reduced anticoagulant effect)
Antipsychotics (impaired anticonvulsant effect)
CYP450 inhibitors (plasma levels increased) – includes isoniazid, diltiazem, verapamil
CYP450 inducers (plasma levels reduced) – includes phenytoin, phenobarbitone, theophylline

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52
Q

what are the contraindications of Carbamazepine

A

Caution in cardiac disease, hepatic or renal impairment, pregnancy, patients with history of haematological reaction to other drugs and those susceptible to angle-closure glaucoma
Avoid in patients with AV conduction abnormalities (if not paced), history of bone marrow depression, acute porphyria and those with know hypersensitivity to tricyclic antidepressants
Discontinue carbamazepine if patients develops acute liver disease or severe/progressive/symptomatic leucopenia

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53
Q

name the brand names of Carbamazepine

A

Tegretol, Temporol, Neurotol

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54
Q

MoA of Citalopram

A

Target: Serotonin re-uptake transporter on the pre-synaptic neuronal membrane
Action: Inhibitor
Effect: Prevents re-uptake and subsequent degradation of the monoamine neurotransmitter serotonin from the synaptic cleft
Overall effect: Prolonged presence of serotonin in the synaptic cleft leads to prolonged neuronal activity – in mood disorders such as depression there are low levels of this neurotransmitter in the brain. SSRIs therefore restore the concentration of serotonin to normal levels.

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55
Q

absorption of Citalopram

A

The bioavailability is 80%

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56
Q

distribution of Citalopram

A

Protein binding is <80%

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57
Q

how is Citalopram metabolised

A

Via the liver via N-demethylation to its main metabolite, demethylcitalopram by CYP2C19 and CYP3A4

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58
Q

how is Citalopram excreted

A

12-23% of an oral dose of citalopram is found unchanged in the urine, while 10% of the dose is found in the faeces

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59
Q

what are the different formulations of Citalopram

A

Tablets, solution

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60
Q

what is the therapeutic indication of Citalopram

A

20 mg once daily, increased in steps of 20 mg daily if required, dose to be increased at intervals of 3–4 weeks; maximum 40 mg per day

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61
Q

what are the side effects of Citalopram

A

GI upset (dose related) – nausea, vomiting, dyspepsia, abdominal pain, diarrhoea, constipation
Anorexia with weight loss
Increased risk of bleeding
Hypersensitivity reactions – rash, urticaria, angioedema, anaphylaxis
Convulsions
Neuroleptic malignant syndrome

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62
Q

what are the interactions of Citalopram

A

Alcohol (increased sedative effect)
NSAIDs (increased risk of bleeding)
Antiepileptics (SSRIs lower the seizure threshold)
Theophylline (half theophylline dose or avoid where possible)
MAOIs – SSRIs should not be started until 2 weeks of stopping an MAOI, MAOIs should not be started until 7-14 days after stopping an SSRI

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63
Q

what are the contraindications of Citalopram

A

Caution in patients with epilepsy (discontinue if convulsions develop), cardiac disease, diabetes mellitus, susceptibility to angle closure glaucoma, history of mania or bleeding disorders, hepatic or renal impairment, those taking other drugs which increase risk of bleeding and those received concomitant electroconvulsive therapy Avoid in pregnancy
Discontinue SSRIs if the patient enters a manic phase

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64
Q

name the brand names of Citalopram

A

Celexa, Cipramil

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65
Q

what is the MoA of Clozapine

A

Target: Muscarinic, histamine, dopamine, serotonin and adrenergic receptors
Action: Mixed antagonists – main action is through antagonism of dopamine D2 receptors
Effect: Reduced release of dopamine from dopaminergic nerve terminals, reduced electrical activity in dopaminergic neuronal pathways – action on mesolimbic/mesocortical pathways is responsible for the antipsychotic activity of these drugs, while action on the nigrostriatal pathways produces the unwanted side effects

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66
Q

what is the absorption of Clozapine

A

Bioavailability is between 60-70%

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67
Q

how is Clozapine excreted

A

80% in metabolized state: 30% biliary and 50% kidney.

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68
Q

how is Clozapine metabolised

A

liver

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69
Q

what are the different formulations of Clozapine

A

Tablets, suspension

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70
Q

what is the therapeutic indication of Clozapine

A

200-450mg daily in divided doses

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71
Q

what are the side effects of Clozapine

A

Drowsiness, sedation; Agitation
Extrapyramidal symptoms; Postural hypotension – risk of falls in the elderly; Tardive dyskinesia (may be irreversible); Neuroleptic malignant syndrome; Agranulocytosis (clozapine only)

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72
Q

what are the interactions of Clozapine

A

Antihypertensive agents (increased hypotensive effect)
Drugs that prolong QT interval (increased risk of arrhythmias including torsades de pointes)
Antiepileptics (lower the seizure threshold)
Opioids (increased CNS depression/sedation) • Alcohol (increased CNS depression)

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73
Q

what are the contraindications of Clozapine

A

Caution in cardiovascular disease, diabetes, Parkinson’s disease and hepatic impairment
Avoid in CNS depression and coma

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74
Q

name the brand names of Clozapine

A

Clozaril, Leponex, Versacloz

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75
Q

MoA of Diazapam

A

Target: Benzodiazepine (BDZ) receptor on GABA-BDZ receptor complex
Action: Agonist
Effect: Increase affinity of the inhibitory neurotransmitter GABA for the GABAA receptor – this causes post-synaptic chloride ion channels to open
Overall effect: Increased flow of negative chloride ions into the neurone leading to hyperpolarisation of the membrane – this prevents further excitation

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76
Q

absorption of Diazapam

A

76% (64–97%) by mouth, 81% (62–98%) recta

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77
Q

distribution of Diazapam

A

Despite high binding to plasma proteins (98-99%) - mainly albumin and to a lesser extent α1-acid glycoprotein - diazepam is widely distributed into tissues and crosses the blood-brain barrier and is highly lipid soluble, which causes the initial effects to decrease rapidly as it is redistributed into fat deposits and tissues

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78
Q

how is Diazapam metabolised

A

via the liver

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79
Q

how is Diazapam excreted

A

kidney

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80
Q

name the different formulations of Diazapam

A

Injection, tablet, solution, gel, emulsion

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81
Q

what is the therapeutic indication of Diazapam

A

Diazepam – 2mg tid increased if necessary to 15-30mg daily in divided doses (half dose in elderly)

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82
Q

what are the side effects of Diazapam

A 
Drowsiness 
Dizziness 
Psychomotor impairment
 Important: 
Hypotension leading to increased risk of falls in the elderly
 Physical and psychological dependence
 Tolerance 
‘Hangover effects’
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83
Q

what are the interactions of Diazapam

A

Antihypertensives (enhanced hypotensive effect) • Clozapine (serious adverse effects reported with lorazepam)

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84
Q

what are the contraindications of Diazapam

A

Caution in the elderly, patients with respiratory disease, muscle weakness, myasthenia gravis (avoid if unstable) and those with a history of drug or alcohol abuse
Avoid in patients with respiratory depression, marked neuromuscular weakness, acute pulmonary insufficiency, sleep apnoea syndrome, pregnancy and breastfeeding
Should not be used for greater than 4 weeks

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85
Q

name the brand names of Diazapam

A

Valium, Vazepam, Valtoco

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86
Q

MoA of digoxin

A

Target: Na+ K + ATPase membrane pump
Action: Inhibitor
Effect: Increase in intracellular sodium. This leads to a subsequent rise in intracellular calcium through the Na+ Ca2+ exchanger on cardiac myocytes. Phases 4 and 0 of the cardiac action potential are prolonged leading to an increase in end diastolic volume.
Overall effect: Positive inotropic effect (increased end diastolic volume leads to increased force of ventricular contraction according to Frank Starling curve), negative chronotropic effect – increases cardiac contractility, decreases heart rate

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87
Q

what is the absorption of digoxin

A

Bioavailability is between 60-80%

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88
Q

what is the distribution of digoxin

A

Protein binding is 25%

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89
Q

what is the metabolism of digoxin

A

liver

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90
Q

how is digoxin excreted

A

kidney

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91
Q

list the different formulations of digoxin

A

Tablet, injection

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92
Q

what is the therapeutic indication of digoxin

A

0.75–1.5mg in divided doses over 24 hours for rapid control of atrial fibrillation or flutter
125–250micrograms daily for maintenance of atrial fibrillation or flutter
62.5-125micrograms daily for heart failure (patient in sinus rhythm) Reduce dose in the elderly and those with renal impairment

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93
Q

what are the side effects of digoxin

A

DIGOXIN TOXICITY: Confusion; Loss of appetite; Nausea, vomiting, diarrhoea; Evidence of cardiotoxicity – palpitations, arrhythmias, conduction disturbances; Blurred or yellow vision If digoxin toxicity is known or strongly suspected and withdrawal of the drug/correction of electrolyte disturbances are ineffective, DIGOXIN-SPECIFIC ANTIBODY FRAGMENTS are indicated.

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94
Q

what are the interactions of digoxin

A

Amiodarone (increased plasma digoxin concentration – halve dose of digoxin)
Calcium channel blockers (increased plasma digoxin concentration)
Drugs which cause hypokalaemia e.g. diuretics increase the risk of cardiotoxicity (secondary to the hypokalaemia

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95
Q

what are the contraindications of digoxin

A

Caution in sick sinus syndrome, hypokalaemia, thyroid disease, severe respiratory disease and in patients who have had a recent MI
Avoid in heart block, Wolff-Parkinson-White syndrome, ventricular tachycardia or fibrillation, myocarditis and constrictive pericarditis Reduce dose in renal impairment

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96
Q

name the brand name of digoxin

A

Lanoxin

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97
Q

what is the MoA of Diltiazem

A

Target: L-type calcium channels - Diltiazem and Verapamil favour the hyperpolarised Ca++ channels more commonly found in cardiac muscle cells
Action: Antagonist
Effect: Inhibit influx of calcium ions into cardiomyocytes through L-type calcium channels
Overall effect: Negative inotropic effect – decreases cardiac contractility

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98
Q

what is the absorption of Diltiazem

A

The bioavailability is 40%

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99
Q

what is the distribution of Diltiazem

A

Protein binding is about 70-80%

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100
Q

how is Diltiazem metabolised

A

the liver

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101
Q

how is Diltiazem excreted

A

Via the kidney and biliary

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102
Q

name the different formulations for Diltiazem

A

Capsule, tablet

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103
Q

what is the therapeutic indication of Diltiazem

A

60mg three times daily, increase if necessary to 360mg daily

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104
Q

what are the side effects of Diltiazem

A

Headache • Flushing • Tachycardia • Peripheral oedema • Constipation, particularly in elderly patients
• Sino-atrial and AV block with diltiazem, particularly in those taking digoxin and/or beta blockers

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105
Q

what are the interactions of Diltiazem

A

Antihypertensives (increased hypotensive effect) • Beta blockers (asystole, severe hypotension, heart failure) • Anti-arrhythmics (increased risk of bradycardia, AV block and myocardial depression)

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106
Q

what are the contraindication of Diltiazem

A

Caution in heart failure, first degree AV block and bradycardia (avoid if severe)
• Avoid in second or third degree AV block, SA block, sick sinus syndrome, Wolff-ParkisonWhite syndrome, hypotension and cardiogenic shock

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107
Q

name the brand names of Diltiazem

A

Cardizem, Dilacorxr,

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108
Q

what is the MoA of Enoxaparin

A

Target: Antithrombin III (a serine protease inhibitor) Action: Activate/stimulate Effect: Inhibit factor Xa in the common pathway of the clotting cascade Overall effect: Factor Xa is needed to convert prothrombin to thrombin, therefore LMWHs inhibit coagulation

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109
Q

what is the absorption of Enoxaparin

A

The absolute bioavailability is 100%

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110
Q

what is the distribution of Enoxaparin

A

Enoxaparin binds to antithrombin III. The percentage of plasma protein binding for enoxaparin is not readily available

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111
Q

how is Enoxaparin metabolised

A

liver

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112
Q

how is Enoxaparin excreted

A

kidney

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113
Q

list the different formulation of Enoxaparin

A

injection

114
Q

what is the therapeutic indication of Enoxaparin

A

Prophylaxis of DVT in surgical patients – 20mg 2 hours before surgery then 20mg every 24 hours (40mg if high risk e.g. orthopaedic surgery)
Prophylaxis of DVT in medical patients – 40mg once daily
Treatment of DVT/PE – 1.5mg/kg once daily
Treatment of acute MI – inital dose 30mg, then 1mg/kg every 12 hours for up to 8 days

115
Q

list the side effects of Enoxaparin

A

Haemorrhage
Heparin-induced thrombocytopenia (HIT)
Hyperkalaemia

116
Q

what is the interactions of Enoxaparin

A

NSAIDs (incerased risk of haemorrhage)
ACE inhibitors, ARBs (increased risk of hyperkalaemia)
Antiplatelet agents (increased risk of haemorrhage)

117
Q

what is the contraindication of Enoxaparin

A

Caution in the elderly, renal impairment,hepatic impairment (avoid if severe) and those with low body weight
Avoid in haemophilia and other haemorrhagic disorders, thrombocytopenia, recent cerebral haemorrhage, severe hypertension, peptic ulcer disease, acute bacterial endocarditis, following major trauma and in patients with known hypersensitivity to heparins
Discontinue if patient develops HIT

118
Q

name the brand names of Enoxaparin

A

Lovenox, Clexane, Xaparin

119
Q

MoA of Haloperidol

A

Target: Muscarinic, histamine, dopamine, serotonin and adrenergic receptors
Action: Mixed antagonists – main action is through antagonism of dopamine D2 receptors
Effect: Reduced release of dopamine from dopaminergic nerve terminals, reduced electrical activity in dopaminergic neuronal pathways – action on mesolimbic/mesocortical pathways is responsible for the antipsychotic activity of these drugs, while action on the nigrostriatal pathways produces the unwanted side effects

120
Q

absorption of Haloperidol

A

The bioavailability is between 60-70% when taken orally

121
Q

what is the distribution of Haloperidol

A

Protein binding is approximately 90%

122
Q

how is Haloperidol metabolised

A

Liver-mediated

123
Q

how is Haloperidol excreted

A

Biliary and in urine

124
Q

list the different formulations of Haloperidol

A

Tablet, solution, injection

125
Q

what is the therapeutic indication of Haloperidol

A

starting dose 0.5starting dose 0.5-3mg 2-3 times daily; maintenance dose 5-30mg daily

126
Q

list the side effects of Haloperidol

A

Drowsiness, sedation; Agitation
Extrapyramidal symptoms; Postural hypotension – risk of falls in the elderly; Tardive dyskinesia (may be irreversible); Neuroleptic malignant syndrome; Agranulocytosis (clozapine only)

127
Q

what are the interactions of Haloperidol

A

Antihypertensive agents (increased hypotensive effect)
Drugs that prolong QT interval (increased risk of arrhythmias including torsades de pointes)
Antiepileptics (lower the seizure threshold)
Opioids (increased CNS depression/sedation)
Alcohol (increased CNS depression)

128
Q

what are the contraindications of Haloperidol

A

Caution in cardiovascular disease, diabetes, Parkinson’s disease and hepatic impairment
Avoid in CNS depression and coma

129
Q

name the brand names of Haloperidol

A

Haldol

130
Q

what sit he MoA of lithium

A

Patients with bipolar affective disorder have diminished GABA neurotransmission. Thus, low GABA levels can result in excitatory toxicity. Lithium increases the levels of GABA which in turn reduces glutamate and down regulates the NMDA receptor. Lithium also directly activates the GABA receptor.

131
Q

what is the absorption of lithium

A
132
Q

what is the distribution of lithium

A

No protein binding

133
Q

how is lithium metabolised

A

Kidney

134
Q

how is lithium excreted

A

> 95% kidney

135
Q

what are the different formulations for lithium

A

Tablets, solution

136
Q

what is the therapeutic indication of lithium

A

Initially 1–1.5 g daily, dose adjusted according to serum-lithium concentration, doses are initially divided throughout the day, but once daily administration is preferred when serum-lithium concentration stabilised.

137
Q

list the side effects of lithium

A

GI upset; Fine tremor; Weight gain
Hypothyroidism
Hyperparathyroidism, hypercalcaemia
Lithium toxicity – blurred vision, muscle weakness, drowsiness, coarse tremor, slurred speech, ataxia, confusion, convulsions, nausea, vomiting and ECG changes If toxicity is suspected:
o Stop lithium immediately
o Check lithium levels, serum creatinine, U&E o Refer to A&E if clinically necessary o Seek advice from psychiatry for re-initiation of lithium

138
Q

what are the interactions of lithium

A

The following drugs increase lithium levels: antibiotics metronidazole, tetracyclines and cotrimoxazole; NSAIDs, ACE inhibitors, ARBs and diuretics
The following drugs decrease lithium levels: xanthines theophyllines, aminophylline and caffeine; sodium salts and acetazolamide
Amiodarone (increased risk of ventricular arrhythmias

139
Q

what are the contraindications of lithium

A

Caution in the elderly and those with psoriasis and myasthenia gravis
Avoid in serious cardiac disease (heart failure, sick sinus syndrome), Addison’s disease, renal impairment (if possible), pregnancy and breastfeeding
Reduce dose or discontinue lithium in diarrhoea, vomiting and intercurrent infection (especially if patient is sweating profusely)
Discontinue lithium 24 hours before surgery and restart as soon as renal function and fluid balance are back to normal

140
Q

what is the brand name of lithium

A
141
Q

what is the MoA of methadone

A

Target: G-protein coupled opioid ‘mu’ receptors in the CNS and peripheral nervous system
Action: Full agonist (high affinity for receptors)
Effect: Closure of N-type voltage-dependent calcium channels and opening of calcium-dependent inwardly rectifying potassium channels – this increases potassium conductance. Opioids also presynaptically inhibit the release of pain-signalling neurotransmitters such as substance P.
Overall effect: Membrane hyperpolarisation and reduced neuronal excitability, reduction or inhibition of pain neurotransmission.

142
Q

what is the absorption of methadone

A

The bioavailability is 15-20% when taken subcutaneously
100% when taken intravenously,
41-99% when taken orally

143
Q

what is the distribution of methadone

A

The protein binding is between 85-90%

144
Q

how is methadone metabolised

A

via the liver

145
Q

how is methadone excreted

A

urine and faeces

146
Q

what is the therapeutic indication of methadone

A

–10 mg every 6–8 hours, adjusted according to response, on prolonged use not to be given more frequently than every 12 hours.

147
Q

what are the side effects of methadone

A 
Nausea/vomiting 
Constipation
Respiratory depression 
Hypotension 
Sedation and coma 
Tolerance 
Physical and psychological dependence
148
Q

what are the interactions of methadone

A

CNS depressants (increased risk of respiratory depression) – alcohol, sedatives, hypnotics, general anaesthetics
MAOIs (potentiate action of morphine)
Alcohol (increased hypotensive and sedative effects)

149
Q

what are the contraindications of methadone

A

Caution in the elderly, hypotension, shock, prostatic hypertrophy, obstructive ir inflammatory bowel disorders, biliary disease, convulsive disorders, adrenocortical insufficiency, hepatic or renal impairment, pregnancy and patients with a history of drug dependence
Avoid in acute respiratory depression, coma, head injury or raised ICP (opioids interfere with pupillary responses used in neurological assessment) and those at risk of paralytic ileus

150
Q

name the brand names of methadone

A

Diskets, Dolophine, Metadol, Metadol-D, Methadose

151
Q

what is the MoA of methotrexate

A

Target: Dihydrofolate reductase enzyme
Action: Competitive inhibitor
Effect: Inhibits reduction of dihydrofolate to its active form tetrahydrofolate
Overall effect: Immunosuppressant activity

152
Q

what is the absorption of methotrexate

A

The bioavailability is between 64-90%

153
Q

what is the distribution of methotrexate

A

Protein binding is between 46.5-54%

154
Q

how is methotrexate metabolised

A

Methotrexate is metabolized by folylpolyglutamate synthase to methotrexate polyglutamate in the liver as well as in tissues. Gamma-glutamyl hydrolase hydrolyzes the glutamyl chains of methotrexate polyglutamates converting them back to methotrexate. A small amount of methotrexate is also converted to 7-hydroxymethotrexate

155
Q

how is methotrexate excreted

A

Methotrexate is >80% excreted as the unchanged drug and approximately 3% as the 7-hydroxylated metabolite.1 Methotrexate is primarily excreted in the urine with 8.7-26% of an intravenous dose appearing in the bile

156
Q

name the different formulations of methotrexate

A

Injection, tablet, solution

157
Q

what is the therapeutic indication of methotrexate

A

dose range 5-25mg once weekly

158
Q

what are the side effects of methotrexate

A

Nausea, diarrhoea
Alopecia
Stomatitis, mucositis
Myelosuppression including leucopenia and neutropenia
Hepatotoxicity
Pulmonary fibrosis, interstitial pneumonitis
Pericarditis, pericardial tamponade

159
Q

what are the interactions of methotrexate

A 
Trimethoprim/co-trimoxazole (risk of pancytopenia, do not co-prescribe) 
NSAIDs (may reduce methotrexate excretion but unlikely to cause clinically significant adverse effects, concomitant use common in rheumatic disease) 
Clozapine (increased risk of agranulocytosis – avoid concomitant use) 
Acitretin (increased plasma methotrexate concentration, increased risk of hepatotoxicity – avoid concomitant use) 
Live vaccines (high risk of infection due to immunosuppressive effect of methotrexate)
160
Q

what are the contraindication of methotrexate

A

Caution in ulcerative colitis, peptic ulcer disease and ulcerative stomatitis
Avoid in pregnancy and breastfeeding, severe hepatic or renal impairment, blood disorders (severe anaemia, leucopenia or thrombocytopenia), untreated folate deficiency and history of alcohol abuse/cirrhosis
Hold methotrexate temporarily if patient is systemically unwell with significant infection requiring anti-infective intervention

161
Q

name the brand names of methotrexate

A

Metoject, Nordimet, Otrexup, Rasuvo, Reditrex, Trexall, Xatmep

162
Q

what is the MoA of phenytoin

A

Target: Voltage-gated neuronal sodium ion channels
Action: Block Effect: Inhibits influx of sodium ion into neuronal cells/slows rate of recovery of sodium channels from inactivation
Overall effect: Stabilises the neuronal membrane and prevents hyperexcitability, thus limiting the spread of seizure activity and reducing seizure propagation

163
Q

what Is the absorption of phenytoin

A

The bioavailability is 70-100%

164
Q

what is the distribution of phenytoin

A

Protein binding is approximately 90% bound

165
Q

how is phenytoin metabolised

A

liver

166
Q

how is phenytoin excreted

A

Urinary 23-70%, bile

167
Q

name the different formulations of phenytoin

A

Capsule, tablet, injection, suspension.

168
Q

what is the therapeutic indication of phenytoin

A

Starting dose – 3-4mg/kg or 150-300mg daily, increased gradually as necessary while monitoring plasma phenytoin concentration Maintenance dose – 200-500mg daily (reduce in hepatic impairment to avoid toxicity)

169
Q

what is the side effects of phenytoin

A 
P= P450 interactions 
H = Hirsutism 
E = Enlarged gums 
N = Nystagmus 
Y = Yellow-browning of the skin
T = Teratogenic 
O = Osteomalacia 
I = Interferes with folate metabolism, leads to anaemia 
N = Neuropathies: vertigo, ataxia, headaches
170
Q

what are the interactions of phenytoin

A

Phenytoin is a cytochrome P450 Inducer
OCP (reduced contraceptive effect)
Theophylline (reduced plasma concentration of both drugs) Cimetidine (reduced plasma phenytoin concentration)
Amiodarone (increased plasma phenytoin concentration)

171
Q

what are the contraindications of phenytoin

A

Caution in patients undergoing enteral feeding
Avoid in patients of Han Chinese or Thai origin (HLA-B*1502 allele increases risk of StevensJohnson syndrome)
Discontinue phenytoin if severe leucopenia develops

172
Q

name the brand names of phenytoin

A

Dilantin, Phenytek

173
Q

what is the MoA of Prednisolone

A

Target: Intracellular steroid receptors
Action: Agonist – prednisolone and other corticosteroids mimic the action of the endogenous mediator cortisol at steroid receptors Effect: Binding of a corticosteroid to the cytoplasmic steroid receptor exposes a DNA binding domain on the receptor. This allows the steroid-receptor complex to associate with glucocorticoid response elements present in the promoter regions of target genes. Overall effect: Upregulation of gene transcription

174
Q

what is the absorption of Prednisolone

A

The bioavailability is 70% when taken orally

175
Q

what is the distribution of Prednisolone

A

Protein binding is between 65-91%

176
Q

how is Prednisolone metabolised

A

liver

177
Q

how is Prednisolone excreted

A

Excreted 98% in the urine

178
Q

name the different formulations of Prednisolone

A

Tablet, ointment cream, suppository, injection, suspension.

179
Q

what is the therapeutic indication of Prednisolone

A

Starting dose – 10-20mg mane after breakfast Maintenance dose – 2.5-15mg daily

180
Q

what is the side effects of Prednisolone

A

Moon face with plethoric cheeks • Steroid induced cataracts • Steroid induced psychosis • Buffalo hump fat distribution • Central fat distribution with striae • Thin limbs with paper money skin and easy bruising • Hypertension • Steroid induced diabetes mellitus

181
Q

what are the interactions of Prednisolone

A

Antihypertensives (reduced hypotensive effect)
NSAIDs (increased risk of peptic ulceration and bleeding) Antidiabetics (reduce hypoglycaemic effect)
Wafarin (may enhance or reduce anticoagulant effect)
Live vaccines – avoid concomitant use due to increased risk of infection

182
Q

what are the contraindications of Prednisolone

A

Caution in pregnancy (risk of intrauterine growth restriction)

183
Q

name the brand names of Prednisolone

A

Millipred Dp 6 Day, Pediapred

184
Q

what is the MoA of Quetiapine

A

Target: Muscarinic, histamine, dopamine, serotonin and adrenergic receptors Action: Mixed antagonists – main action is through antagonism of dopamine D2 receptors Effect: Reduced release of dopamine from dopaminergic nerve terminals, reduced electrical activity in dopaminergic neuronal pathways – action on mesolimbic/mesocortical pathways is responsible for the antipsychotic activity of these drugs, while action on the nigrostriatal pathways produces the unwanted side effects

185
Q

what is the absorption of Quetiapine

A

The bioavailability is 100%

186
Q

what is the distribution of Quetiapine

A

The protein binding 83%

187
Q

how is Quetiapine metabolised

A

Liver via CYP3A4-catalysed sulfoxidation to its active metabolite norquetiapine

188
Q

how is Quetiapine excreted

A

Kidney 73% faeces- 20%

189
Q

what is the formulation of Quetiapine

A

Tablets, capsule

190
Q

what are the side effects of Quetiapine

A

Drowsiness, sedation; Agitation

191
Q

what is the therapeutic indication of Quetiapine

A

25 mg twice daily for day 1, then 50 mg twice daily for day 2, then 100 mg twice daily for day 3, then 150 mg twice daily for day 4, then, adjusted according to response, usual dose 300–450 mg daily in 2 divided doses, the rate of dose titration may need to be slower and the daily dose lower in elderly patients; maximum 750 mg per day.

192
Q

what are the interactions of Quetiapine

A

Antihypertensive agents (increased hypotensive effect)
Drugs that prolong QT interval (increased risk of arrhythmias including torsades de pointes)
Antiepileptics (lower the seizure threshold)
Opioids (increased CNS depression/sedation)
Alcohol (increased CNS depression)

193
Q

what are the contraindications of Quetiapine

A

Caution in cardiovascular disease, diabetes, Parkinson’s disease and hepatic impairment
Avoid in CNS depression and coma

194
Q

name the brand name of Quetiapine

A

Seroquel

195
Q

what is the MoA of Rivaroxaban

A

Target: Factor Xa
Action: Competitive inhibition
Effect: Inhibits activated factor Xa, which is required for the conversion of prothrombin to thrombin in the common pathway of the coagulation cascade
Overall effect: Lack of thrombin prevents conversion of fibrinogen to fibrin and therefore inhibits thrombus formation

196
Q

what is the absorption of Rivaroxaban

A

The bioavailability is between 80-100%

197
Q

what is the distribution of Rivaroxaban

A

Protein binding is between 92-95%

198
Q

how is Rivaroxaban metabolised

A

CYP3A4, CYP2J2 and CYP-independent mechanisms

199
Q

how is Rivaroxaban excreted

A

Liver

200
Q

what is the different formulations of Rivaroxaban

A

Tablets, capsule, suspension

201
Q

what is the therapeutic indication of Rivaroxaban

A

10mg once daily for 2 weeks to be started 6-10 hours after surgery

202
Q

what are the side effects of Rivaroxaban

A 
Nausea 
Renal impairment (rivaroxaban)
203
Q

what are the interactions of Rivaroxaban

A 
NSAIDs (increased risk of bleeding) 
Amiodarone (increased plasma dabigatran concentration – reduce dose of dabigatran) 
Verapamil (increased plasma dabigatran concentration – reduce dose of dabigatran) 
Triazole antifungals (avoid combination with rivaroxaban)
204
Q

what are the contraindications of Rivaroxaban

A

Caution in the elderly, patients weighing <50kg, active or recent GI ulceration and those with bleeding disorders
Avoid in active bleeding and in severe renal or hepatic impairment, pregnancy and breast feeding.
Discontinue if severe bleeding occurs

205
Q

name the brand name of Rivaroxaban

A

Xarelto

206
Q

what is the MoA of Sildenafil

A

Sildenafil is an oral therapy for erectile dysfunction. The physiological mechanism responsible for the erection of the penis involves the release of nitric oxide (NO) in the corpus cavernosum during sexual stimulation
Nitric oxide then activates the enzyme guanylate cyclase, which results in increased levels of cyclic guanosine monophosphate (cGMP), producing smooth muscle relaxation in the corpus cavernosum and allowing inflow of blood.

207
Q

what is the absorption of Sildenafil

A

The bioavailability is 41%

208
Q

what is the distribution of Sildenafil

A

Protein binding is approximately 96%

209
Q

how is Sildenafil metabolised

A

liver

210
Q

how is Sildenafil excreted

A

Faeces and urine

211
Q

list the different formulations of Sildenafil

A

Tablet, injection, suspension

212
Q

what is the therapeutic indication of Sildenafil

A

For pulmonary arterial hypertension:
Oral: 20mg 3x a day
Injection: 10mg 3x a day
For erectile dysfunction: initially 50mg approx. 1 hour before sexual activity, adjusted accordingly to response 25-100mg as required. To be taken as a single dose maximum one dose a day.

213
Q

what are the side effects of Sildenafil

A

Alopecia; anaemia; anxiety; cough; diarrhoea; dizziness; fluid retention; gastrointestinal discomfort; gastrointestinal disorders; headaches; increased risk of infection; insomnia; nasal complaints; nausea; night sweats; pain; skin reactions; tremor; vasodilation; vision disorders

214
Q

what are the interactions of Sildenafil

A
215
Q

what are the contraindications of Sildenafil

A

Hereditary degenerative retinal disorders; history of non-arteritic anterior ischaemic optic neuropathy; recent history of myocardial infarction; recent history of stroke
When used for Erectile dysfunction
avoid if systolic blood pressure below 90 mmHg (no information available); patients in whom vasodilation or sexual activity are inadvisable; recent unstable angina
When used for Pulmonary arterial hypertension: sickle-cell anaemia

216
Q

name the brand name of Sildenafil

A

Revatio, Viagra, Vizarsin

217
Q

what is the MoA for Sodium Valproate

A

Target: Voltage-gated sodium channels
Action: Inhibitor Effect:Inhibit inactivation of inhibitory neurotransmitter GABA and block its reuptake into neurones
Overall effect: Inhibition of action potential transmission both pre- and post-synaptically, leading to increased levels of GABA in the brain and interruption of seizure activity

218
Q

what is the absorption for Sodium Valproate

A

Rapid absorption

219
Q

what is the distribution for Sodium Valproate

A

Protein binding is between 80-90%

220
Q

how is Sodium Valproate metabolised

A

via the liver

221
Q

how is Sodium Valproate excreted

A

via the urine

222
Q

list the different formulations of Sodium Valproate

A

Injection, tablet, syrup, capsule

223
Q

what is the the therapeutic indication for Sodium Valproate

A

Starting dose – 600mg daily in 1-2 divided doses, increase by 200mg every 3 days Maintenance dose – 1-2g daily (reduce in renal impairment)

224
Q

what is the side effects for Sodium Valproate

A

GI disturbance (nausea, gastric irritation, diarrhoea) • Weight gain • Drowsiness
Thrombocytopenia
Pancreatitis
Hyperammonaemia
Reduced bone mineral density
Hepatic dysfunction (including fatal hepatic failure)

225
Q

what are the interactions for Sodium Valproate

A

Antidepressants (reduced anticonvulsant effect) – SSRIs, TCAs, MAOIs
Antimalarials (reduced anticonvulsant effect) – mefloquine, chloroquine

226
Q

what are the contraindications for Sodium Valproate

A

Caution in renal impairment and systemic lupus erythematosus
Avoid in active liver disease, hepatic impairment, pregnancy and in patients with family history of severe hepatic dysfunction
Discontinue if patient develops abnormally prolonged prothrombin time, pancreatitis, blood disorder or hepatic dysfunction

227
Q

name the brand names for Sodium Valproate

A

Depakene, Depakote, Epival

228
Q

what is the MoA for Spironolactone

A

Target: Intracellular aldosterone receptors (mineralocortocoid receptors (MR)) in the renal tubules
Action: Competitive antagonist, blocks adosterone-MR translocation into the nucleus reducing the production of aldosterone induced proteins (AIPs)
Effect: Inhibits Na+ /K+ exchange in the distal tubule and collecting ducts, promoting potassium retention and sodium and water loss
Overall effect: Weak diuresis, potassium retention and hypotensive effect

229
Q

what is the absorption for Spironolactone

A

The bioavailability is between 60-80%

230
Q

what is the distribution for Spironolactone

A

Protein binding is 88% to albumin

231
Q

how is Spironolactone metabolised

A

liver

232
Q

how is Spironolactone excreted

A

Urine and in bile

233
Q

list the different formulations for Spironolactone

A

Tablet, capsule

234
Q

what is the therapeutic indication for Spironolactone

A

Ascites: 50mg twice daily (increase to 200mg twice daily if required) Heart failure 25mg once daily

235
Q

what are the side effects for Spironolactone

A

GI upset
Hyperkalaemia
Gynaecomastia/hypogonadism, impotence in males, menstrual irregularities in females (due to cross-reaction with intracellular androgen receptors)
Acute renal failure

236
Q

what are the interactions for Spironolactone

A

Drug affecting RAAS (increased risk of hyperkalaemia) – ACE inhibitors, ARBs, direct renin inhibitors
Other potassium sparing diuretics e.g. amiloride, triamterene (increased risk of hyperkalaemia)
Potassium supplements
Antihypertensives (increased hypotensive effect)
NSAIDs (increased risk of nephrotoxicity)
Lithium – excretion is inhibited by spironolactone

237
Q

what are the contraindications for Spironolactone

A

Caution in the elderly and those with renal impairment (avoid if severe)
Avoid in hyperkalaemia, hyponatraemia, anuria and Addison’s disease

238
Q

name the brand names for Spironolactone

A

Aldactazide, Aldactone, Carospir

239
Q

what is the MoA of Tamoxifen

A

Tamoxifen competitively inhibits oestrogen binding to its receptor, which is critical for it’s activity in breast cancer cells.1 Tamoxifen leads to a decrease in tumour growth factor α and insulin-like growth factor 1, and an increase in sex hormone binding globulin. The increase in sex hormone binding globulin limits the amount of freely available estradiol.1 These changes reduce levels of factors that stimulate tumour growth.

240
Q

what is the absorption of Tamoxifen

A

The bioavailability is approximately 100%

241
Q

what is the distribution of Tamoxifen

A

The protein binding of tamoxifen in plasma is over 98% and mostly to serum albumin

242
Q

how is Tamoxifen metabolised

A

Hepatic

243
Q

how is Tamoxifen excreted

A

Faeces and urine

244
Q

name the different formulations of Tamoxifen

A

tablet

245
Q

what is the therapeutic indication for Tamoxifen

A

For adult, initaly 20mg on days 2,3,4,5 of cycle. If necessary the daily dose may be increased to 40mg then 80mg for subsequent courses. If cycle is irregular, start initial course on any day, with subsequent course starting 45 days later or on day 2 of cycle if period occurs

246
Q

what are the adverse effects of Tamoxifen

A

Alopecia; anaemia; cataract; cerebral ischaemia; constipation; diarrhoea; dizziness; embolism and thrombosis; fatigue; fluid retention; headache; hepatic disorders; hot flush; hypersensitivity; hypertriglyceridaemia; muscle complaints; nausea; neoplasms; retinopathy; sensation abnormal; skin reactions; taste altered; uterine disorders; vaginal haemorrhage; vomiting; vulvovaginal disorders

247
Q

what are the interactions for Tamoxifen

A

Acenocoumarol and warfarin ( increases anticoagulant effect), buproin and cinacalcet and fluoxetine ( decrease the efficacy) fosphenytoin- high dose might increase the cocncentration of fosphenytoin

248
Q

what are the contraindications for Tamoxifen

A

Void if you have a history of getting DVT

249
Q

name the brand names for Tamoxifen

A

Nolvadex-D, Soltamox

250
Q

what is the MoA for Temazepam

A

Target: Benzodiazepine (BDZ) receptor on GABA-BDZ receptor complex
Action: Agonist
Effect: Increase affinity of the inhibitory neurotransmitter GABA for the GABAA receptor – this causes post-synaptic chloride ion channels to open
Overall effect: Increased flow of negative chloride ions into the neurone leading to hyperpolarisation of the membrane – this prevents further excitation

251
Q

what is the absorption of Temazepam

A

The bioavailability is approximately 96%

252
Q

what is the distribution for Temazepam

A

96% of unchanged temazepam is bound to plasma proteins

253
Q

how is Temazepam metabolised

A

via the liver

254
Q

how is Temazepam excreted

A

via the kidney

255
Q

name the different formulations for Temazepam

A

Capsule, solution, suppositry

256
Q

what is the therapeutic indication for Temazepam

A

10–20 mg once daily, alternatively 30–40 mg once daily, higher dose range only to be administered in exceptional circumstances, dose to be taken at bedtime, for debilitated patients, use elderly dose.
For elderly dose:
10 mg once daily, alternatively 20 mg once daily, higher dose only to be administered in exceptional circumstances, dose to be taken at bedtime.

257
Q

what are the side effects for Temazepam

A 
Drowsiness 
Dizziness 
Psychomotor impairment
Hypotension leading to increased risk of falls in the elderly 
Physical and psychological dependence 
Tolerance 
‘Hangover effects’
258
Q

what are the interactions for Temazepam

A

Antihypertensives (enhanced hypotensive effect)

Clozapine (serious adverse effects reported with lorazepam)

259
Q

what are the contraindication for Temazepam

A

Caution in the elderly, patients with respiratory disease, muscle weakness, myasthenia gravis (avoid if unstable) and those with a history of drug or alcohol abuse
Avoid in patients with respiratory depression, marked neuromuscular weakness, acute pulmonary insufficiency, sleep apnoea syndrome, pregnancy and breastfeeding
Should not be used for greater than 4 weeks

260
Q

name the brand name of Temazepam

A

Restoril

261
Q

what is the MoA for warfarin

A

Target: Vitamin K epoxide reductase
Action: Competitive inhibitor
Effect: Prevents post-translational gamma-carboxylation clotting factors II, VII, IX and X
Overall effect: Depletion of active clotting factors II, VII, IX and X; this produces a potent anticoagulant effect

262
Q

what is the absorption for warfarin

A

Bioavailability is between 79-100%

263
Q

what is the distribution for warfarin

A

Protein binding is 99%

264
Q

how is warfarin metabolised

A

liver

265
Q

how is warfarin excreted

A

Kidney

266
Q

what are the formulation of warfarin

A

Injection, tablet, solution

267
Q

what is the therapeutic indication of warfarin

A

Loading dose 5-10mg
Daily maintenance dose 3-9mg at the same time each day
Dose depends on patient’s prothrombin time (INR), wide interindividual variation in dose

268
Q

what are the side effects of warfarin

A

Haemorrhage
Skin necrosis
Hypersensitivity

269
Q

what are the interactions of warfarin

A 
enhances anticoagulant effects:
NAIDs including aspirin
anti-arrhythmias eg amiodarone 
antibacterials- chloramphenicol 
anti fungals 
lipid lowering drugs 
ulcer healing drugs 
reduces anti coagulant effects:
antieplieptics 
antifungals 
oral contraceptives 
vitamin k 
retinoids 
antidepressants
270
Q

what are the contraindications of warfarin

A

Caution in patients who have undergone recent surgery, those taking other druigs which increase the risk of bleeding and those with renal impairment (avoid if severe)
Avoid in pregnancy, peptic ulcer disease, severe hypertension and those with hepatic impairment (especially if prothrombin time already prolonged)

271
Q

name the brand names of warfarin

A

Coumadin, Jantoven

272
Q

what is the MoA for Zopiclone

A

these drugs bind with high selectivity to the α1 subunit of the GABAA receptor/chloride ion channel complex. As such they have strong hypnotic activity but negligible anxiolytic, myorelaxant and anticonvulsant properties. They are for short term use only (up to 4 weeks).

273
Q

what is the absorption of Zopiclone

A

The bioavailability is between 75-80%

274
Q

what is the distribution of Zopiclone

A

Protein binding is between 52-59%

275
Q

how is Zopiclone metabolised

A

hepatic

276
Q

how is Zopiclone excreted

A

urine

277
Q

name the different formulations of Zopiclone

A

tablet

278
Q

what is the therapeutic indication of Zopiclone

A

For adults 7.5 mg once daily for up to 4 weeks, dose to be taken at bedtime.
For elderly Initially 3.75 mg once daily for up to 4 weeks, dose to be taken at bedtime, increased if necessary to 7.5 mg daily.

279
Q

what are the side effects of Zopiclone

A

Dry mouth, `anxiety, dizziness. Confusion

280
Q

what are the interactions of Zopiclone

A

Antihypertensives (enhanced hypotensive effect)

Clozapine

281
Q

what are the contraindications of Zopiclone

A

Marked neuromuscular respiratory weakness; myasthenia gravis; respiratory failure; severe sleep apnoea syndrome
Don’t take while pregnant and breastfeeding
Don’t drive while taking this medication or using heavy machinery as can make you feel drowsy

282
Q

name the brand names of Zopiclone

A

Imovane

year 3 (11 decks)

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