I M Ar 2 Flashcards
Amiodarone mechanism
Blocks sodium, calcium, potassium channels
Antagonism of a/b adrenergic receptors
Amiodarone adverse effects during IV infusion
Hypotension
Amiodarone adverse effects when taken chronically
Pneumonitis, bradycardia, hepatitis, photo sensitivity, thyroid abnormalities
Who shouldn’t take amiodarone
Severe hypotension
Heart block
Thyroid disease
Amiodarone interactions
Increase plasma conc of digoxin, diltiazem, verapamil
Prescription of amiodarone needs
Senior involvement (f1 not on own)
Amiodarone for cardiac arrest
300mg followed by flush
If repeated IV of amiodarone indicated how is it administered? Why?
Central line
Peripheral can cause phlebitis
Why should you not copy the preceding dose on prescription of amiodarone
May be a loading dose
ACEi egs
Ramipril, lisinopril, perindopril
ACEi uses
Hypertension
Chronic heart failure / ischemic heart disease
Diabetic nephropathy / CKD with pronteinuria
Mechanism of ACEi
Presents conversion of angiotensin I -> II
ACEi adverse effects
Hypotension (can be profound after first dose)
Dry cough
Hyperkalaemia
Cause / worsen renal failure (especially with renal artery stenosis)
Rarely - angiodema , anaphylaxis
Wh should not get ACEi
Renal artery stenosis
Acute kidney injury
Pregnant / breastfeeding
Chronic kidney disease (use lower dose)
ACEi interactions
Avoid potassium elevating drugs
NSAIDs -> increas risk of renal failure
How are ACEi prescribed - dose
Usually around 2.5mg daily titrated up to 10mg over few weeks
Dose of ramipril for heart failure / neohropathy
1.25mg daily
What to tell patients getting ACEi
Dizzy - especially after first dose Dry cough Tell someone if allergic signs Avoids NSAIDs eg ibuprofen Will need blood test monitoring
What should be checked before starting ACEi
Electrolytes and renal functions
Angiotensin receptor blockers egs
Losartan, candesartan, irbesartan
ARBs uses
Hypertension
Chronic heart failure / ischemic heart disease
Diabetic nephropathy / CKD with pronteinuria
ARBs mechanism
Block action of angiotensin II on AT1 receptor
ARBs adverse effects
Hypertension (especially first dose)
Hyperkalaemia
Renal failure
Why do ARBs not cause a dry cough
Do not affect ACEi (involved in bradykinin metabolism )
-> also less likely to cause angiodema
Who should not get ARBs
Renal artery stenosis
Acute kidney injury
Pregnant / breastfeeding
CKD - use lower doses
ARBs interactions
Don’t use with potassium elevating drugs
Risk of renal failure with NSAIDs
Prescription on ARBs
50mg orally daily titrated up
Losartan in heart failure
Start on 12.5mg daily
What to tell patients getting ARBs
Dizziness
Will need blood test monitoring
Avoid taking NSAIDs
What should be checked before starting ARBs
Electrolytes and renal function
In what ethnic group are ARBs preferable to ACEi
Black African / Caribbean as risk of angiodema is 5x higher then general population with ACEi
SSRIs egs
Citalopram
Fluoxetine
Sertraline
Escitalopram
SSRIs uses
Moderate - severe depression (mild if other treatments fail)
Panic disorder
OCD
SSRIs mechanism
Inhibit neuronal reputable of serotonin
Why are SSRIs generally preferred to tricyclics
Fewer adverse effects and less dangerous in overdose
SSRIs adverse effects
GI upset, weight / appetite disturbance Hypersensitivity Suicidal thoughts Lower seizure threshold Can prolong QT interval -> arrythmias Increase risk of bleeding Serotonin syndrome
What is serotonin syndrome
Autonomic hyperactivity
Altered mental state
Neuromuscular excitation
When should you be cautious of precribing SSRIs
Epileptics
Peptic ulcer disease
Young people
Hepatic impairment (as metabolised)
Which drugs should not be given with SSRIs ? Why?
Monoamine oxidase inhibitors (also increase serotonin -> serotonin syndrome risk)
Drugs that prolong QT interval eg. Antipsychotics
Carful with aspirin / NSAIDs (due to bleeding risk)
Prescribing SSRIs (citalopram)
20mg orally daily increased as needed
What to tell patient getting SSRIs
May need psychological therapy for longer term benefits
Carry on with SSRIs for 6 months after feel better
Not to stop suddenly -> tummy upset, flu like symptoms
Which SSRIs have fewer interactions
Citalopram and escitalopram
Tricyclics egs
Amitriptyline
Lofepramine
Tricyclics indications
Moderate - sever depression when SSRIs don’t work
Neuropathic pain
Tricyclics mechanism
Inhibit neuronal reuptake of serotonin and noradrenaline
Tricyclics mechanism which causes adverse effects
Block muscarinic, H1, A1/2, D2 receptors
Triclyclics adverse effects ? (Receptor blocked)
Dry mouth, constipation, urinary retention, blurred vision (antimuscarinic).
Sedation, hypotension (a1/H1).
Arrythmias, ECG changes.
Convulsions, hallucinations, mania.
Breast changes sexual dysfunction, extra pyramidal eg tremor / dyskinesia (dopamine)
Sudden withdrawal of tricyclics causes
GI upset, flu like
Who should tricyclics be used with caution
Elderly, CV disease, epilepsy, constipation, prostatic hyper trophy, raised intraoccular pressure
Which drugs should not be given with tricyclics
Mono amine oxidase inhibitors
Amytriptyline dose for neuropathic pain? Depression?
10mg at night
75mg daily
What needs to be thought about when prescribing tricyclics
Very dangerous in overdose -> prescribe small quantity at a time
What to tell patients getting tricyclics
Takes a few weeks for symptom improvement
May need psychological therapy
Keep taking for 6 months after better
Don’t stop suddenly
Amiodarone uses
Tachyarrythmias (usually when other treatments none suitable)
What to tell patients getting tricyclics
Will improve symptoms over a few weeks.
May need psychological therapy for long term benefits.
Keep taking for 6months after symtoms improve
Don’t stop treatment suddenly -> flu like withdrawal
Venlafaxine and mirtazepine uses
Major depression (SSRIs not effective) generalised anxiety disorder (venlafaxine only)
Mechanisms of venlafaxine and mirtazapine
Increase availability of monoamines for neurotransmisson
Venlafaxine and mirtazapine adverse effects
GI upset
CNS effects - headache, abnormal dreams, convulsions….
Less common - hyponatraemia, serotonin syndrome
Venlafaxine and mirtazapine sudden withdrawal ->
GI upset and flu like symptoms
Venlafaxine and mirtazapine caution with who?
Elderly, hepatic /renal impairment, Cv disease (Venlafaxine associated with arrythmias)
Venlafaxine and mirtazapine interactions
SSRIs -> serotonin syndrome
Prescribing venlafaxine and mirtazepine
Low dose titrated up
V - 37.5 twice daily up to 375 daily
M- 15mg daily up to 45
Venlafaxine and mirtazapine tell patients
Improve symptoms over a few weeks
May need psychological therapy
Keep taking for 6 months after improvement
Not stop taking suddenly
Egs of d2 receptor antagonists (antiemetics)
Metoclopramide , domperidone
What is the main receptor in the chemoreceptor trigger zone
D2
D2 antagonist uses
Nausea and vommiting - especially in reduced gut motility
D2 antagonists adverse effects
Diarrhoea (as promoted gastric emptying)
Short term - acute dystonic reaction
Extra pyramidal symptoms
D2 antagonist - who is more likely to get extra pyramidal symptoms
Children and young adults
Prokinetic effects of d2 antagonists mean they are contraindicated in who
GI obstruction / perforation
Risk of extra pyramidal symtoms increases with metoclopramide and what other class
Antipsychotics (same mechanism)
Metoclopramide antagonises effect of what drugs (contraindicated)
Dopaminergic agents for Parkinson’s
Starting dose for metoclopramide and domperidone
10mg three times daily
Eg of h1 antagonist antiemetics
Cyclizine, cinnarizine, promethazine
H1 antiemetics uses
Nausea and vommiting - especially with motion sickness or vertigo
H1 antagonist antiemetics mechanism
Block h1 receptors in vomiting centre and communication with vestibular system
H1 antiemetics adverse effects
Drowsiness
Dry throat and mouth
Tachycardia (palpitations)
Warnings with h1 antagonist antiemetics
Prostatic hyper trophy (antimuscarinic may lead to retention) Hepatic encephalopathy (due to sedation)
Eg of phenothiazines (antiemetics)
Prochlorperazine
Chlorpromazine
Phenothiazines uses
Nausea and vomiting especially with vertigo
Psychotic disorders
Phenothiazines mechanism
Mostly by d2 antagonist in vomiting centre and vestibular system
Phenothiazines adverse effects
Drowsiness Postural hypotension Extrapyramidal symptoms Short term - acute dystonic reaction QT prolongation
Who should not get phenothiazines
Sever liver disease - never
Prostatic hyper trophy - retention
Elderly
Which drugs interact with phenothiazines
Any that prolong QT
Antipsychotics, amiodarone , Ciproflaxacin, macrolides, quinine, SSRIs
Egs of 5HT-3 antagonists
Ondansetron, granisetron
5HT3 antagonists mechanism
High amount of 5ht3 receptors in chemoreceptor trigger zone.
Serotonin also key transmitter in gut
5ht3 antagonists warning
Prolong QT interval at high doses
Avoid other drugs that do this
Drugs that prolong QT
Antipsychotics, amiodarone , Ciproflaxacin, macrolides, quinine, SSRIs, phenothiazines, 5ht3 antagonists
Prescription of ondansetron
4-8mg every 12 hours
Antiemetics potential for morning sickness as minimal risk to baby
Ondasetron
Antifungals egs
Nystatin, clotrimazole, fluconazol
What is found in fungal membranes but not human cells and therefore target of antfungals
Ergosterol
Nystatin / clotrimazole adverse effects
Local irritation where applied
Fluconazole adverse effects
GI upset, headache, hepatitis
Rarely - prolonged QT
Fluconazole contraindications
NEVER in pregnancy - malformations
Liver disease / renal impairment
Interactions with fluconazole
Any metabolised by P450 (as inhibits)
Drugs that prolong QT
Eg of drugs metabolised by p450
Phenytoin, carbamazepine, warfarin, diazepam, simvastatin, sulphonyureas
How is nystatin usually prescribed
Oral suspension for oral candidiasis
Cream for skin infections
How is clotrimazole prescribed? What for ?
Cream
Tinea (ringworm ), candidia
H1 antagonist uses
Allergies
Relieve pruritus, urticaria
Anaphylaxis (after adrenaline)
Nausea and vomiting
Antihistamines eg
Cetirizine, loratadine, fexofenadine, chlorphenamine
Which cells release histamine
IgE
Which antihistamine causes some sedation? Why do others (2nd gen) not ?
Chlorphenamine
Others don’t cross blood brain barrier
Who should not get get chlorphenamine
People with severe liver disease
Eg of anti motility drugs
Loperamide, codeine phosphate
Anti motility used to treat
Diarrhoea
Anti motility mechanism
Agonist of opioid u receptors in GI.
So transit of bowel contents + increase anal sphincter tone
When should loperamide not be used
Acute UC / C. difficile as increases risk of mega colon.
Dysentery - as likely bacterial infection
Usual dose of loperamide
4mg followed by 2mg after each lose stool
What to tell patient getting loperamide
Treats diarrhoea but not underlying cause
Eg of bronchodilator muscarinics
Ipatropium, Tiotropium, glycopyrronium
Uses of bronchodilators
COPD p, asthma
Mechanism of bronchodilators
Competitive inhibitor of acetyl choline
-> reduce smooth muscle tone / secretions
Bronchodilators adverse effects
Dry mouth
Bronchodilators caution in
Patients susceptible to angle-closure glaucoma
Which bronchodilators are short acting / long
Short - ipatropium
Long - tiotropium / glycopyrronium
What needs to be monitored with bronchodilators
Inhaler technique
Anti muscarinics for GI / cardio uses egs
Atropine, hyoscine butyl bromide, glycopyrronium
What is atropine used to treat
Bradycardia
First line treatment for IBS
Hyoscine butyl bromide
What is used to treat copious respiratory secretions
Hyoscine butyl bromide
Mechanism of GI / cV antimuscarinics
Competitive inhibitor of acetyl choline
Increase heart rate, reduce smooth muscle tone, reduce secretions
Adverse effects of GI / cv antimuscarinics
Tachycardia, dry mouth, constipation, urinary retention, blurred vision, drowsiness and confusion
Who should antimuscarinics be cautious with
Susceptible to angle-closure glaucoma
Arrythmias
Preciption of atropine for bradycardia
300-600 micrograms every 2 minutes until acceptable heart rate
Antimuscarinics for IBS prescription
10mg 8 hourly (hyoscine butyl bromide )
GU antimuscarinic egs
Oxybutynin, tolterodine, solifenacin
Which receptor are GU antimuscarinics selective (ish) for
M3 - promotes bladder relaxation
Adverse effects of GU antimuscarinics
Dry mouth, tachycardia, constipation, blurred vision
When should GU antimuscarinics be avoided
Never in UTI
Cautious in elderly, angle-closure glaucoma, arrythmias, urinary retention
What should be done before prescribing antimuscarinics for urge incontinence
Adequate bladder training
Eg of first gen antipsychotics
Haloperidol, chlorpromazine, prochlorperazine
1antipsychotics uses
Psychomotor agitation, schizophrenia , bipolar, nausea and vomiting
Mechanism of 1antipsychotics
Block post synaptic d2
3 dopaminergic pathways in CNS
Mesolimbic / mesocortical - midbrain and limbic / frontal cortex.
Nigrostriatal - substantia nigra and corpus striatum (basal ganglia).
Tuberohypophyseal - hypothalamus and pituitary
Main drawback / adverse effect of 1antipsychotics ? Which pathway ?
Extrapyramidal effects - movement abnormalities from blockade of d2 in nigrostriatal
Types of Extrapyramidal in 1antipsychotics
Acute dystonic reactions - Parkinsonism movements / spasms.
Akathisia - state of inner restlessness.
Neuroleptic malignant syndrome - confusion, autonomic disregulation and pyrexia (life threatening)
Tardive dyskinesia - (late onset) pointless repetitive movements eg. Lip smacking
Which Extrapyramidal symptom may not stop after stopping treatment
Tardive dyskinesia
Adverse effects of 1amtipsychotics
Extrapyramidal
Drowsiness, hypotension, QT prolongation, erectile dysfunction, hyperprolactinaemia
When should you be cautious of 1antipsychotics
Elderly - start lower dose
Dementia
Parkinson’s - due to Extrapyramidal
Drug interactions with 1 antipsychotics
Any that prolong QT
Second gen antipsychotics egs
Quetiapine, olanzapine, risperidone, clozapine
2antipsychotic uses
Psychomotor agitation
Schizophrenia
Bipolar
Mechanism of 2antipsychotics
Block post synaptic d2 receptors
Main adverse effect of 2antipsychotics
Metabolic disturbance - weight gain, diabetes
2antipsychotic adverse effects
Sedation, Extrapyramidal, metabolic disturbance, prolong QT, sexual dysfunction / breast symptoms
Clozapine specific adverse effect
1% agranulocytosis (deficiency of neutrophils
Myocarditis
Clozapine not used in which patients
Neutropenia
Severe heart disease
2antipsychotics caution in ?
Cv disease
2antipsychotics interactions
Should not be combined with dopamine blocking antiemetics / drugs that prolong QT