Pharmacology P3 Flashcards

1
Q

Complications of opioid misuse:

A
  • 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
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2
Q

Emergency management of opioid overdose:

A

IV or IM naloxone - rapid onset and short duration of action

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3
Q

Management of opioid dependence:

A

methadone or buprenorphine

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4
Q

Effect of organophosphate poisoning on receptors:

A
  • inhibition acetylcholinesterase
  • upregulation of nicotinic and muscarinic cholinergic neurotransmission
  • sarin gas similar
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5
Q

Features of organophosphate poisoning:

A

(SLUD)

  • Salivation
  • Lacrimation
  • Urination
  • Defecation
  • Cardiovascular - hypotension, bradycardia
  • small pupils, muscle fasciculation
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6
Q

Management of organophosphate poisoning:

A

atropine

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7
Q

Management of paracetamol poisoning basic:

A
  • activated charcoal if <1 hour ago
  • NAC
  • liver transplant
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8
Q

Management of salicylate poisoning basic:

A
  • urinary alkalisation with IV bicarbonate

- haemodialysis

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9
Q

Management of benzodiazepine overdose basic:

A

flumazenil

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10
Q

Management of TCA overdose basic:

A

IV bicarbonate

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11
Q

Management of lithium overdose basic:

A
  • volume resuscitation
  • haemodialysis
  • sodium bicarbonate
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12
Q

Management of methanol poisoning basic:

A
  • fomepizole or ethanol

- haemodialysis

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13
Q

Management of iron overdose basic:

A
  • desferrioxamine

- chelating agent

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14
Q

Management of lead poisoning basic:

A
  • dimercaprol

- calcium edetate

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15
Q

Management of cyanide overdose basic:

A
  • hydroxycobalamin

- combination of amyl nitrite, sodium nitrite and sodium thiosulfate

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16
Q

Inducers of P450 system:

A
  • phenytoin, carbamazepine
  • barbiturate: phenobarbitone
  • rifampicin
  • St John’s wort
  • chronic alcohol intake
  • griseofulvin
  • smoking
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17
Q

Inhibitors of P450 system:

A
  • ciprofloxacin, erythromycin
  • isoniazid
  • cimetidine, omeprazole
  • amiodarone
  • allopurinol
  • ketoconazole, fluconazole
  • SSRI: fluoxetine, sertraline
  • ritonavir
  • sodium valproate
  • acute alcohol intake
  • quinupristin
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18
Q

When should acetylcysteine be given in paracetamol overdose?

A
  • 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
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19
Q

How is NAC given and what is a possible reaction?

A
  • infused over 1 hour to reduce ADR
  • causes anaphylactoid reaction - non-IgE mediated mast cell release
  • stop transfusion and restart at slower rate
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20
Q

Criteria for liver transplantation in paracetamol liver failure:

A
  • arterial pH <7.3 24 hours after ingestion

- OR PT >100sec + creatinine >300micromol/L + grade III or IV encephalopathy

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21
Q

Who is at increased risk of developing hepatotoxicity following paracetamol overdose:

A
  • taking liver enzyme inducing drugs
  • malnourished patients
  • acute alcohol intake is protective
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22
Q

What is first pass metabolism and what drugs does this apply to?

A
  • 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
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23
Q

What is zero-order kinetics and what drugs exhibit this?

A
  • metabolism is independent of concentration of reactant
  • metabolic pathway becomes saturated
  • phenytoin, salicylates (e.g. high dose aspirin), heparin, ethanol
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24
Q

What are examples of phosphodiesterase type V inhibitors and how do they work?

A
  • 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
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25
Contraindications to PDE5 inhibitors:
- taking nitrates and related drugs e.g. nicorandil - hypotension - recent stroke or MI (wait 6 months)
26
Side effects of PDE5 inhibitors:
- visual disturbance: blue discolouration, non-arteritic anterior ischaemic neuropathy - nasal congestion - flushing - GI side effects - headache - priapism
27
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
28
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
29
How do aldosterone antagonists like spironolactone work?
- act in cortical collecting duct | - used for ascites, heart failure, nephrotic syndrome and Conn's syndrome
30
Drugs to avoid in renal failure:
- antibiotics: tetracycline, nitrofurantoin - NSAIDs - lithium - metformin
31
Drugs likely to accumulate in CKD so need dose adjustment:
- most antibiotics - digoxin, atenolol - methotrexate - sulphonylureas - furosemide - opioids
32
Drugs harmful in pregnancy:
- tetracyclines - aminoglycosides - sulphonamides and trimethoprim - quinolones - ACEi and ARBs - statins - warfarin - sulfonylureas - retinoids - cytotoxics - antiepileptics
33
What are quinolone and how do they work?
- inhibit DNA synthesis and are bactericidal - e.g. ciprofloxacin and levofloxacin - inhibit topoisomerase II and topoisomerase IV
34
ADR of quinolones and CONTRA:
- lower seizure threshold - tendon damage - cartilage damage - lengthens QT interval - avoid in pregnancy and breastfeeding and G6PD
35
What is the acid base balance like in salicylate overdose:
- early stimulation of respiratory centre leads to respiratory alkalosis - later on, the acid effects of salicylates lead to metabolic acidosis
36
Features of salicylate overdose:
- hyperventilation - tinnitus - lethargy - sweating, pyrexia - nausea and vomiting - hyperglycaemia and hypoglycaemia - seizures - coma
37
Indications for haemodialysis in salicylate overdose:
- serum conc >700mg/L - metabolic acidosis resistant to treatment - acute renal failure - pulmonary oedema - seizures - coma
38
Causes of serotonin syndrome:
- MAOI - SSRI - St John's wort can interact - ecstacy - amphetamines
39
Features of serotonin syndrome:
- neuromuscular excitation: hyperreflexia, myoclonus, rigidity - ANS excitation: hyperthermia, sweating - altered mental state: confusion
40
Management of serotonin syndrome:
- IV fluids - benzodiazepines - serotonin antagonists e.g. cyprohepatidine or chlorpromazine
41
Side effects ACEi:
- cough | - hyperkalaemia
42
Side effects bendroflumethiazide:
- gout - hypokalaemia - hyponatraemia - impaired glucose tolerance
43
Side effects calcium channel blockers:
- headache - flushing - anke oedema
44
Side effects beta blockers:
- bronchospasm - fatigue - cold peripheries
45
Side effects doxazosin:
postural hypotension
46
Side effects amoxicillin:
rash with infectious mononucleosis
47
Side effects co-amoxiclav:
cholestasis
48
Side effects flucloxacillin:
cholestasis after a few weeks
49
Side effects erythromycin:
- GI upset | - prolonged QT
50
Side effects ciprofloxacin:
- lowers seizure threshold | - tendonitis
51
Side effects metronidazole:
reaction with alcohol
52
Side effects doxycycline:
photosensitivity
53
Side effects trimethoprim:
- rashes - photosensitivity - pruritus - suppression of haematopoiesis
54
Side effects sulfonylureas:
- hypoglycaemia - increased appetite and weight gain - SIADH - liver dysfunction
55
Side effects glitazones:
- weight gain - fluid retention - liver dysfunction - fractures
56
Side effect gliptins:
pancreatitis
57
What is St John's wort:
- as effective as TCA in mild-moderate depression | - similar MOA to SSRI
58
ADR St John's wort:
- serotonin syndrome - inducer of P450 system - effectiveness of COCP reduced
59
What is tamoxifen and how is it used?
-SERM -oestrogen receptor antagonist and partial agonist -oestrogen receptor positive breast cancer -used for 5 years following tumour removal (raloxifene is pure antagonist and carries lower endometrial cancer risk)
60
ADR tamoxifen:
- menstrual disturbance: bleeding, amenorrhoea - hot flushes - VTE - endometrial cancer
61
What teratogenic effect do ACEi have:
- renal dysgenesis | - craniofacial abnormalities
62
What teratogenic effect does alcohol have?
craniofacial abnormalities
63
What teratogenic effect do aminoglycosides have?
ototoxicity
64
What teratogenic effect does carbamazepine have?
- NTD | - craniofacial
65
What teratogenic effect does chloramphenicol have?
grey baby syndrome
66
What teratogenic effect does cocaine have?
- IUGR | - preterm labour
67
What teratogenic effect does diethylstilbestrol have?
vaginal clear cell adenocarcinoma
68
What teratogenic effect does lithium have?
Ebstein's anomaly
69
What teratogenic effect do tetracyclines have?
discoloured teeth
70
What teratogenic effect does thalidomide have?
limb reduction
71
What teratogenic effect does warfarin have?
craniofacial abnormalities
72
How do you treat theophylline toxicity?
- activated charcoal regardless of time - haemodialysis - IV crystalloid for hypotension - diazepam for seizures - IV beta blockers for SVTs - antiemetics
73
Normal lithium therapeutic range:
0.4-1.0mmol/L
74
TCA overdose features:
- anticholinergic: dry mouth, dilated pupils, agitation, sinus tachycardia, blurred vision - severe: arrhythmias, seizures, metabolic acidosis, coma
75
ECG changes with TCA overdose:
- sinus tachy - QRS >100ms - seizures - QRS >160ms - ventricular arrhythmias
76
MOA and ADR of rifampicin:
- inhibits bacterial DNA dependent RNA polymerase and prevents DNA to mRNA transcription - potent liver enzyme inducer, hepatitis, orange secretions, flue like symptoms
77
MOA and ADR of isoniazid:
- inhibits mycolic acid synthesis - peripheral neuropathy: prevent with pyridoxine - hepatitis, agranulocytosis - liver enzyme inhibitor
78
MOA and ADR of pyrizinamide:
- converts pyrazinamidase into pyrazinoic acid which in turn inhibits fatty acid synthase - hyperuricaemia causing gout - arthralgia, myalgia - hepatitis
79
MOA and ADR of ethambutol:
- inhibits enzyme arabinosyl transferase which polymerises arabinose into arabinan - optic neuritis: check visual acuity before and during