Pharmacology/Toxicology Flashcards
Drug induced thrombocytopenia
Quinine
Abciximab
NSAIDs
Furosemide
Abx - penicilins, sulphonamides,
rifampicin
Anticonvulsants - Carbamazepine, Valproate
Heparin
Carbon monoxide affect on O2
Causes decreased O2 saturation of Hb - - > LEADS TO EARLY PLATEAU
Ciclosporin side effects
EVERYTHING INCREASED:
BP Gums Hair K+ Fluid
Pharmacokinetic terms :
Half life
Volume of distribution
Half life = time taken for plasma drug conc to decrease by half
Volume of distribution - calue that descibes the extent at which a drug is retained within circulation or distributed elsewhere.
Pharmacodynamic termsL:
Efficacy
Emax
Potency
a measure of drug effects in a particular symptom
Emax - maximal effect - partial agonist Emax < Full agonist
Potency: Expresses drug efficacy in relation to dose/conc.
Pharmacokinetics - Metabolism
2 types of biochemical rxn:
Phase 1:
- oxidation/reduction/hydrolysis.
- P450
- toxic/reactive product
Phase 2:
- Conjugation
- products less reactive
- typical groups - glucoronyl/acetyl/methyl/sulphate
1st pass metabolism:
- Drug is extensively etaboliused before reaching systemic circulation.
in LIVER
- ASA, verapamil, GTN, Propanolo, ISMN, hydrocortisone, testosterone
Zero-order kinetics:
- Metabolism is independent of drug conc.
- Metaboplic pathway= saturated
- Phenytoin, ASA, Heparin, Ethanol
Drug induced lupus
Assoc with Acetylation and HLA-DR4
Ft:
- butterfly rash
- myalgia
- pleurisy
Causes:
- PROCAINAMIDE
- HYDRALAZINE
- others: isoniazid, phenytoin, minocyclione
Inx:
- ANA +,/ dsDNA -
- anti-histone Ab
Liver inducers/inhibitors
inducers - stop warfarin - PCBRAS
- Pghenytoin/carbamezapine/barbituates/rifampicin/alcohol/St Johns wort
Inhibitors - inc warf - AODEVICES
- allopurinol/omeprazole/disulifram./erythromycin/valproate/isoniazid/ciproflox/ethanol/sulfonamide
Fx of COCP
decreased absopriton - e.g. diarrhoea
Liver inducers
Con-comitant broad-spec Abx
drugs to avoid in pregnancy
Earyl - teratogenics:
- Li - cardiac abnormalities
- ACEI/ARBs - oligohydraminos
- phenytoin - cleft lip/palate
- Na Valp - NT Defects/spina bifida
- Warfarin
Late preg –> X placents:
- Carbimazole –> neonatal goitre
- Gentamycin - CN8 deafness
prescribing in BReastfeeding
- Amiuodarone
- n Cytotoxics
- Gold
- Indometacin
- Li
- Iodides
- OEstrogens
Liver Fx
Increase susceptible to sedatives/ drugs taht cause encephalopathy
Thiazide/loop diuretics –> hypokalaemia –> Encephalopathy
Rifampicin - accumulates as excreted in bile
Hypoalbuminaemia –> Phenytoin toxicirty
Poor clotting –> Warfarin leads to bleed
NSAIDs - Inc NA/H2O retention
Cardiology drugs
Abciximab - glycoprotein 3a/2b inhibitor –| platelet aggregation
Adenosine - activates K+ in SAN/AVN - CI - Asthma
Aliskiren - Direct renin inhibitor - used in essential HTN
- S.e High K+
Amiodarone:
- prolongs refractory period
- long half life
- give IV - effect hrs
- PO effect = weeks
- it is the LEAST NEG INOTROPIC ANTIARRHYTHMIC
\s.e. - CHIPCHANGE - cutaneous photosensitivity/hep dysfn/inc LDL/pulm fibrosis/CNS/hypo/hyper-thyrid/asx corneal deposits/neuropathy/GI effect/ Enhanced warf and dig
ACEI:
- CI - BL RAS
- S.e. - dry cough/hyperkalaemia/hypersesnsitivity
Clopidogrel:
- Inhibits ADP bindiong site on platelet - stopp aggregation
- P2Y12
- longer anti-plt than ASA –> bleeding risk for 7/7
Digoxin:
- Slows AVN conduction –> Blsacks Na/K+ ATPasa pumo
- eliminated by KIDNEYS
- S.e. –> Gynaecomastia
Flecainide:
- class 1c anti-arrythmic
- avoid if IHD/structural heart dx
Statins:
- HMG CoA reductase inhib –> inhib RLS of cholesterol synth
- S.E. - myopathy/drug induced hepatitis
Ivabradine_
- Funny current blocker - inward NA-K channel - found in SAN
- S.e - visual effects, headache, bradycardia/HB
Nicorandil:
- V.D. used in angina
- activates K+ Channels –> inc. cGMP
- S.E. - headache, flushing, ulceration
- CI - LVF
Pasugrel/Tocagrelor:
- P2Y12 receptor inhibitor
- use Ticagrelor in ANY NSTEMI
s. e. - bleeding/ brady + inc SOB (ticagrelor)
Thiazide:
- hypo Na/K/Mg
- hypochloraemic acidossis
- postural hypotension
- agranulocytosis
- pancreatitis
- thrombocytopenia
Digoxin toxicity
- reverse tick
- arrythmias
- confusion
- yellow-green vision
precipitants:
- hypokalaemia - competively competes with dig
- low MG / High Ca
- Inc Age/ RFx/
- MI
- Drugs 0- amiodarone/verapamil/ dilitiazerm
Mx:
[- Digi-bind
- correct arrythmioa
- Monitor K+
Endocrinology - Drugs
Carbimazole:
- inhibits peroxidase enzyme
- Agranulocytosis
- X placenta –> neonatal goitre/hypothyrpoid.
HRT:
- reduces bone fracture
- inc breast Ca
NAteglinide/repaglinide:
- INCREASE INSULIN secretion
- similar mechanism as SU
- good for postprandial hyperBGL as short 1/2 line
- S.e> - GI Upset/hypersensitivity rxn
GAstro - drugs
S-ulfasalazine:
- S- afe in oregnancy ]- pro -drug of 5-ASA –> dec neutrophil chemotaxis/lymphocyte prolif/pro inflamm cytokines.
- cuation w/ G6PD deficiency or allergy to aspirin/sulkphonamides.
S.e. - oligospermia/SJS/ pneumonitis/lung fibrosis. myelosupression/heinz body anaemia/ coloured tears
Mesalazine/Osalazine:
- types of 5-ASA
- S>E - GI Distrubance / headache/pancretitis
Orlistat:
- Inhibits pancreatic lipase
- used ij obesity if BMI >30 or BMI > 28 + RF or cont WL
PArkinsons meds - See neuro notes
MAO-B inhib - Selegline
Amantadine - inhibit reuptake of DA
L-DOPA
- absorbed in prox. small bowel - decr. if AA present
- prodrug
- netabolised by COMT
- S.e. - Arrythmia/dyskinesia/post lowBP /psychosis/somnolescence
DA-R agonisst:
- Carbegoline/bromocriptine/apomorphine/ropinerole - less dyskinesia vs L-DOPA
- inc neuro psych s.e. ]
- pulm/retroperitoneal fibrosis
Epilepsy meds
lamotrigine
- inhibits glutamate
- s.e. mood change/mavulopapular rash/influenza symptoms/SJS
Gabapentin:
- GABA isomer
Leviteracetam
- presynaptic GABA release
Vigabatrin
- irreversible inhib of GABA transaminase –> inc GABA activity
BZD:
- inc affinity for GABA to bind to it’s receptor
Carbamezapine:
- derivative of TCA:
- HEadache/diplopia soon after starting ]
- morbilliform rash
- toxic epidermal necrolysis
- AGRANULOCYTOSIS
Valproate - S.e = V.A.L.P.R.O.A.T.E
- Vomitting/allopecia/liver toxicity/pancytopaenia or pulm fibrosis/ retention of fat = wG/ pedema/ataxia/ teratogenic or tremor/ enzyme inhib.
- AGRANULOCYTOSIS
5 HT - agonist:
- Triptans
- used in acute migraine
0- do not give in 24 hr of hemiplegic migraine or egotamine –> Vasospasm
- S.e. - chest paibn, flushing, drowsiness, vasospasm
Rheumatology drugs
MTX:
- Folate agonist - inhibits dihydrofolate mediators
- 1st kline in RA
- S.e. - Pulm fibrosis /mucositis/myelosupression.pneumonitis/liver fibrosis
- m Preg - avoid for 6/12
- monitor FBC/U+E/LFT - @ start –> wkly until stable –> every 2-3/12
- interactions - Trimethoprim/co-trimoxazole –> marrow supressionm
- ionteractions - high dose ASA –> inc toxicity
- MX toxicity with folic acid
Allopurinol:
- Inhibits xanthine oxidase –> stops purne synth
- inc risk of acute attach on commencent
- can cause accum of azathiprine
- decrease clearance of cyclophosphamide
Colchicine:
- Inhibits macrophage migration
- s.e. –> diarrhoea
Febuxostat:
- Xanthine oxidase inhibitor.
TOXICITY BEAR
LOOK UP PIC
Azathiprine - neurotoxic Cisplatoin - ototoxic and nephrotoxic Doxyrubicin - Cardiotoxic PSI - cyclophosphamide - bladdeer toxic MTX - Nephrotoxic/myelosupression Vincristine - periph neuropathy Vincristine 0- periph neuropathy
Retinoids
usewd in sev psoriasis/acne
Teratogenic --> NT Defect 0 S.e.: - Benign IHH - dry mucus memrban e - PHOTOSENSITIVITY - decreased night vision
Strontium
used in post-menopauesal osteoperosis
S.e.:
- Sev Allergy
DRESS - drug rash w/ eosinophillia and systemic sx
Spec drug adverse effects
Amennorhgea:
- DA block - chlorpromazine, cimetidine
- Na Valproate
Bronchospasm
- ASA
- BSAIDs
- Adenosine
- beta blkocker
Dyskineasia:
- L- DOPA > other antiparkinsons
Gynaecomastia:
- OEstrogen like - Dig/ spiro
- anti-androgen –> LHRH analogue/cimetidine
Drug induced liver dx
Heoatocellular:
- Paracetamol
- Valproate
- MAOI
- Halothane
- anti-TB - R.I.P
- statins
- Alcohol/amiodarone
Cholestasis: - COCP - Fluclox / erythomycin / co-amox - anabolic . steroids - chlorpromazine/promethazine -
Liver Cirrhosis
- MTX
- amiodarone
- methyldopa
drug provoked myasthenia
amenoglycloside beta block phenytoin penicillamine procaiamide lidocaine
drug induced photosensitivity
Amiodarione Tetracyclines RETINNOIDS PSoralen Cipro
drug induced vasculiuti s
allopurinol \Catopril Cimetidine LTRA penicillin
acute pancreatitis - drug causes
antiretrovirals azathiprine corticosteroidn fibrates statins thiazides
SIADH - derug causaes
Carbamazepine
chlorpropamide
cytotoxic
PAracetamol OD
liver normally conjugats paractamol + glutathione
in OD –> saturated –> all glutatjione used. Therefore get oxidation of P450 mixed fn oxidases. –> toxic metabolite = N- Acetly - B - Benziquinoneimine.
Mx:
- <1hr –> aCharcoal
- > 1hr/staggered –> NAC
- at 4hrs if level >100 –> NAC
- @15hrs >15 –> NAC
S.e of NAC:
- Anaphylactoid rxn –> STOP and restart @ SLOWER rate.
Kings college criteria:
- Arterial pH <7.3
or All of :
- Cr >300
- PT <100
- Encephalopath grade 3/4
TCA OD
Amitriptyline + dosulepin
Early sx:
- dry mouth
- blurred vision
- sinus tachy
- agitation
- blurred pupil
Ft of sev poisoning:
- Arrythmias
- Seizures
- Metabolic acidosis
- Coma
ECG Changes:
- Tachy
- Wide QRS - >100 - seizures >140 –> VT
- prolonged QT
Mx:
- IV NaHCO3-
- IV lipid emulsion
Throphylline toxicity
Sev acidosis
Tachy
Hypokalaemia
LOC/seizures/confusion
MX:
- Rpt aCharcoal
- IVI
- Electrolyte
- if level >60 !!! –> HAEMODYALISis