Pharmacology P3 Flashcards
Complications of opioid misuse:
- viral infection due to sharing needles: HIV, hep B and C
- bacterial - infective endocarditis, septic arthritis, septicaemia, necrotising fasciitis
- VTE
- respiratory depression and death
- psychological
- social
Emergency management of opioid overdose:
IV or IM naloxone - rapid onset and short duration of action
Management of opioid dependence:
methadone or buprenorphine
Effect of organophosphate poisoning on receptors:
- inhibition acetylcholinesterase
- upregulation of nicotinic and muscarinic cholinergic neurotransmission
- sarin gas similar
Features of organophosphate poisoning:
(SLUD)
- Salivation
- Lacrimation
- Urination
- Defecation
- Cardiovascular - hypotension, bradycardia
- small pupils, muscle fasciculation
Management of organophosphate poisoning:
atropine
Management of paracetamol poisoning basic:
- activated charcoal if <1 hour ago
- NAC
- liver transplant
Management of salicylate poisoning basic:
- urinary alkalisation with IV bicarbonate
- haemodialysis
Management of benzodiazepine overdose basic:
flumazenil
Management of TCA overdose basic:
IV bicarbonate
Management of lithium overdose basic:
- volume resuscitation
- haemodialysis
- sodium bicarbonate
Management of methanol poisoning basic:
- fomepizole or ethanol
- haemodialysis
Management of iron overdose basic:
- desferrioxamine
- chelating agent
Management of lead poisoning basic:
- dimercaprol
- calcium edetate
Management of cyanide overdose basic:
- hydroxycobalamin
- combination of amyl nitrite, sodium nitrite and sodium thiosulfate
Inducers of P450 system:
- phenytoin, carbamazepine
- barbiturate: phenobarbitone
- rifampicin
- St John’s wort
- chronic alcohol intake
- griseofulvin
- smoking
Inhibitors of P450 system:
- ciprofloxacin, erythromycin
- isoniazid
- cimetidine, omeprazole
- amiodarone
- allopurinol
- ketoconazole, fluconazole
- SSRI: fluoxetine, sertraline
- ritonavir
- sodium valproate
- acute alcohol intake
- quinupristin
When should acetylcysteine be given in paracetamol overdose?
- if staggered overdose or doubt over time of ingestion regardless of plasma conc
- plasma conc is on or above treatment line regardless of risk factors of hepatotoxicity
How is NAC given and what is a possible reaction?
- infused over 1 hour to reduce ADR
- causes anaphylactoid reaction - non-IgE mediated mast cell release
- stop transfusion and restart at slower rate
Criteria for liver transplantation in paracetamol liver failure:
- arterial pH <7.3 24 hours after ingestion
- OR PT >100sec + creatinine >300micromol/L + grade III or IV encephalopathy
Who is at increased risk of developing hepatotoxicity following paracetamol overdose:
- taking liver enzyme inducing drugs
- malnourished patients
- acute alcohol intake is protective
What is first pass metabolism and what drugs does this apply to?
- concentration of drug is greatly reduced before it reaches systemic circulation due to hepatic metabolism
- larger oral dose needed
- aspirin, isosorbide dinitrate, GTN, lignocaine, propranolol, verapamil, isoprenaline, testosterone, hydrocortisone
What is zero-order kinetics and what drugs exhibit this?
- metabolism is independent of concentration of reactant
- metabolic pathway becomes saturated
- phenytoin, salicylates (e.g. high dose aspirin), heparin, ethanol
What are examples of phosphodiesterase type V inhibitors and how do they work?
- vasodilation through increase in cGMP leading to smooth muscle relaxation in blood vessels supplying corpus cavernosum
- sildenafil (viagra) - short acting (1 hour before)
- tadalafil - longer acting, take on regular
- vardenafil
- also used to manage pulmonary hypertension
Contraindications to PDE5 inhibitors:
- taking nitrates and related drugs e.g. nicorandil
- hypotension
- recent stroke or MI (wait 6 months)
Side effects of PDE5 inhibitors:
- visual disturbance: blue discolouration, non-arteritic anterior ischaemic neuropathy
- nasal congestion
- flushing
- GI side effects
- headache
- priapism
What are the potassium sparing diuretics:
- epithelial sodium channel blockers: amiloride and triamterene
- aldosterone antagonists: spironolactone and eplerenone
- caution if taking ACEi as they precipitate hyperkalaemia
How does amiloride work?
- blocks epithelial sodium channels in distal convoluted tubule
- weak diuretic, given with thiazides or loop diuretics as alternative to potassium supplementation
How do aldosterone antagonists like spironolactone work?
- act in cortical collecting duct
- used for ascites, heart failure, nephrotic syndrome and Conn’s syndrome
Drugs to avoid in renal failure:
- antibiotics: tetracycline, nitrofurantoin
- NSAIDs
- lithium
- metformin
Drugs likely to accumulate in CKD so need dose adjustment:
- most antibiotics
- digoxin, atenolol
- methotrexate
- sulphonylureas
- furosemide
- opioids