Pharmacology COPY Flashcards
Azathioprine s/e
Marrow suppression
Hepatotoxic
Diarrhoea and nausea
Pancreatitis
Carbamazepine side effect
Carb - carbs make you Gain weight and hope your fat cos of a baby!
Maze - makes you dizzy, nausea, low Na
Pine - wish I had neutrophils (agranulocytosis and aplastic anaemia)
Rash most common (SJS in Chinese HLA)
Also decreases effect of OCP
Valproate inhibits metabolism of some drugs causing toxicity
Phenobarbitone, phenytoin, lamotrigine
Pancreatitis, LfTs, alopecia, weight gain
Topiramate side effects
To Lose Weight
Nephrolithiasis, glaucoma, weight loss
Lamotrigine increased by
Valproate and decreased by CMZ
Rash SJs
Vigabactrin side effect
V=Visual field loss, reduced night vision (permanent)
Brachial plexus at what level causes horners
T1
Bell’s palsy loss of taste where
Anterior tongue
SE interferon
Flu like, BM suppression, alopecia
SE ribavirin
Haemolytic anaemia, teratogenic
SE of cyclosporine
Hirsutism most common
Renal HTN Liver toxicity GI upset Tremor Parasthesias Gingival hyperplasia
Calcineurin inhibitor (stops IL2)
Hydroxychloroquine monitoring
Eye 6 monthly
PK
Dose to achieve concentration
PD
Concentration-response relationship
Steady state is
Rate in = rate out
(Reached after 5 half lives)
a drug infused at a constant rate reaches about 94% of steady state after 4 half lives
Beta lactam pr scribing important principle
Time above MIC
Aminoglycosides mechanism of action
Inhibition of protein synthesis
Thiopentone mechanism of action
Potentiates action of GABA
Ketamine and neonate
Neuronal apoptosis and long term memory deficits
Stilboesterol long term effect
Vaginal carcinoma
Tetracycline long term effect
Teeth staining
Neuroleptic malignant syndrome
a life-threatening, neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs. Symptoms include high fever, sweating, unstable blood pressure, stupor, muscular rigidity, and autonomic dysfunction
ACEi cough mediated by
Bradykinin
NO mechanism of action
SM relaxation by up regulation cGMP
Codeine path enzyme required
CYP2D6
CYP450 inhibitors and inducers
Inhibitors only MAC (macolides, antifungals, CCB - verapamil, diltiaem) and grapefruit juice
Inducers all the others
RASS (rifampicin, anti-seizure - phenobarb, phenytoin, carbamazepine, St. John’s wort)
Ondansetron
Serotonin 5HT-3 antagonist
Reversal drug for benzo
Flumazenil
Statins
Statins areHmG-CoA reductase inhibitors
MMF/metformin/SSRI most common se
GI disturbance
Valproate and phenytoin in pregnancy effects
Valproate NTD
Phenyt fetal hydantoin syndrome
Pancuronium does it cross placenta
No - used in LsCS
Bioavailability worked out wth
AUC
Rituximab mechanism of action
Anti CD20 antibody
Citalopram ECG change
Prolonged QT
Mechanism of action of methylphenidate and amphetamine
Block reuptake of dopamine
Mechanism of action of atomoxetine
Selective NA reuptake inhibitor
Blocks transporter and blocks reuptake ofNA
Prevelance OCD
1%
Pimecrolimus classification and s/e
Celcineurin inhibitor (immune mediated anti inflammatory)
Burning and increase infection
Not atrophy
Main concerning side effect of propranolol
Hypoglycaemia
Sirolimus
mTOR inhibitors (inhibits cell growth and angiogenesis)
Omalizumab
Anti IgE antibody
UVA or B used
B because A is risk skin ca
Sotalol side effects
Bradycardia, lethargy, QT prolonged
Flecainide side effects
Tingling, constipation, blurred vision, monitor blood levels
Side effect digoxin
Hypokalaemia
Frusemide action site
Loop diuretic acting on loop of henle
Thiazides diuretic site of action
Proximal and distal tubules
Spironolactone site of action
Aldosterone antagonist acts on distal tubule
Contraindication to diuretics, b blocker, acei, calcium channel blocker
Diuretics - gout
Beta blocker - asthma, diabetes
Ace inhibitors - pregnancy, bilateral renal artery stenosis, high potassium
Calcium channel blocker- heart block
Drug that can worsen pulm HTN
Contraceptives
Statins mechanism of action
HMG-CoA reductase inhibitors
Statins side effects
Commonly GI/headache/myalgia Sleep disturbed and nightmares Memory loss Myopathy Interstitial lung disease Deranged lfts CK up Rhabdo
Other treatments apart from statins (2)
Nicotinic acid (B3) imcreases HDL cholesterol Ezetimibe is cholesterol absorption inhibitor
Other than tamiflu what can you use > 5 year olds?
Zanamavir is another neuraminidase inhibitor, delivered as an inhaled powder by rotadisk. It is active against influenza A and B, sometimes even for strains resistant to Oseltamivir. It is licensed for children >5years. Treatment dose is 2 x 5mg inhalations twice daily for 5 days; prophylaxis dose is 2x 5mg inhalations once daily for 10 days.
Tamiflu reduces sx by 1 day
AED highest risk SJS
LTG
AED in pregnancy
Lamotrigine
AED mostly renal excreted
Levetiracetam and gabapentin
Halve digoxin dose if prescribed with
Amiodarone
Sotalol must monitor
QT interval
Stimulants in ADHD mechanism of action
Methyphenidate and amphetamine
– Block reuptake of dopamine
Amphetamine
– Increases dopamine release
Atomoxetine
– Blocks transporter and blocks reuptake of
noradrenalin
Tacrilomus SE
Burning topically
tremor, renal impairment, hyperglycaemic conditions, diabetes mellitus, hyperkalaemia, infections, hypertension and insomnia.
Can check levels
MMF most common side effect
GI
Name three teratogens in pregnancy
Carbamazepine (Nt defect)
Valproate (nt defect)
MTX (CNS defects)
Carbimazole (hypothyroidism) so PTU preferred
Quinine (deafness)
Toluene (similar to fetal alcohol syndrome)
Misoprostol (moebius sequence with facial paralysis)
Steroid ? Cleft
Warfarin teratogenic effect
Nasal hypoplasia
Cyclophosphamide adverse effects
Gametogenesis affected
Increased risk secondary tumours (DNA damaged)
Haemorrhaging cystitis
Bleomycin side effect
Pulmonary toxicity (fibrosis usually dose related and delayed )
Vinca alkaloids bind to tubulin in M phase and inhibits mitosis
Side effects
Neurotoxic (peripheral neuropathy)
Intrathecal vincristine fatal
CisPLATINUM and carboPLATINUM side effects
Dose related ototoxicity and renal toxicity
Neurotoxic
What drug can worsen liver failure in underlying metabolic disease
Sodium valproate
Infliximab mechanism of action
Neutralises TNFa by binding to it and stopping it attaching to receptors
Vasopressin in vwd mechanism
Increases release of vwf from endothelial cells
Pulmozyme (dornase alfa) mechanism of action
Hydrolyses DNA in mucus (recombinant human deoxyribonuclease I)
Isotrenitoin in pregnancy causes
Facial, ear, heart deformities
Methotrexate 80% excrete by? And what can interfere and cause toxicity
Renal
Aciclovir, allopurinol, PPI some abx
Ribavirin side effect
Haemolytic anaemia
Thromboxane is a powerful vasodilator or vasoconstrictor
Vasoconstrictor
Antidiuretic hormone mechanism
Inserts aquaporins into apical membrane
ACEi side effects
Risk hyperkalaemia
Paracetamol overdose physiology
Broken into toxic metabolite by cytochrome p450 and binds to glutathione
Most likely condition to respond to SSRI
Anxiety
Oral rehydration contains starch for
Fermentation
And ORT with zinc reduces diarrhoea too
C peptide level to see
Amount of insulin
The drugs that most commonly cause SJS/TEN are:
Sulfonamides: cotrimoxizole;
Beta-lactam: penicillins, cephalosporins
Anti-convulsants: lamotrigine, carbamazepine, phenytoin, phenobarbitone
Allopurinol
Paracetamol/acetominophen
Nevirapine (non-nucleoside reverse-transcriptase inhibitor)
Nonsteroidal anti-inflammatory drugs (NSAIDs) (oxicam type mainly)
Second generation H1 receptor antagonists effectively relieve most of the symptoms of allergic
rhinoconjunctivitis.
Which one of the following symptoms is least effectively relieved?
A. Nasal congestion.
B. Nasal itch.
C. Ocular tearing.
D. Rhinorrhoea.
E. Sneezing.
A
The cough associated with the use of angiotensin-converting enzyme (ACE) inhibitors is mediated through
Bradykinin
Non competitive antagonist
non-competitive antagonist binds to a receptor irreversibly and cannot be displaced by an agonist
Clearance formula
CL = Vd * Ke/half life
[Ke = elimination constant=0.7]
CL = volume of distribution/half life
CL in L/h (check units!)
Half life formula
t1/2 = Vd/CL
Check units
What is high first pass metabolism
What route isn’t first pass metabolised
1: when drug uptake by Gut into liver system before goi into blood and high amount metabolised so minimal active drug in system
2: nasal
Volume of distribution is
theoretical volume that would be necessary to contain the total amount of an administered drug at the same concentration that it is observed in the blood plasma.
The distribution of drug in body or plasma after dose
Which anti epileptic is most teratogenic
Valproate
But others include CMZ, phenobarbital and phenytoin
Tricyclics overdose Tx
Sodium bicarbonate
Rituximab mechanism of action
Inhibits CD20
G6PD drugs to avoid (3)
Nitrofurantoin
Methylene blue
Rasburicase
Primaquine
On antipsychotics and present with fever, coma, rigid muscles and autonomic dysfunction
Called?
Neuroleptic malignant syndrome
First order kinetics
K is a constant and first order kinetics the same fraction or percentage is eliminated at a rate (therefore a log)
What drug can go into zero order kinetics
Phenytoin
Aspirin can bind to platelets no upregulation receptors
Bioequality of a drug percent
AUC and peak conc Cmax 80-125%
Red man syndrome with what drug
Vancomycin (related to rate of administration)
Carbamazepine genetics HIGH risk SJs
Asian carbamazepine HLAB1502 HIGH risk SJS
Renal stones SE
Topirimate
Tachyphylaxis is
The more drug you add it becomes less effective
sotalol mechanism and SE
(blocks potassium
channels, can cause bradycardia and lethargy and prolongs QT),
Flecinide SE
Blurred vision, tingling, constipation
Need trough levels
Drugs causing prolonged QT
AAA TakesCare of your Ford Engine
Antihistaminics Anticholinergics Antiarrythmics (specially Quinidine and Sotalol) TCAS Fluoroquinolones Erythromycin
antibiotics (erythromycin, clarithromycin, cotrimoxazole), antifungal agents (fluconazole), antiprotozoal agents, antihistamines (selected), antidepressants (tricyclics), antipsychotics (haloperidol, risperidone, chlorpromazine), antiarrhythmic drugs, lipid lowering
Gum hyperplasia, ataxia, hirsute, nystagmus what drug
Phenytoin
Cyclizine and metoclopramide mechanism of action
Cyclizine = H1 receptor antagonist Met = dopamine receptor antagonist
Thioliazines and metformin action
Increase sensitivity to insulin
Metformin also suppresses liver glucose production
Sulfonylurea (gliclazide) action
Increased secretion
Exposed valproate teratogen risk NTD
1-2%
Carbimazole mechanism of action
Blocking iodisation and coupling of tyrosine molecules on thyroglobulin
Diazoxide mechanism of action
potent openers of the K+ ATP channels present on the insulin producing beta cells of the pancreas.
Valproate SE
V.A.L.P.R.O.A.T.E Vomiting Alopecia/ammonia Liver toxicity Pancreatitis/ Pancytopenia Retention of fats (weight gain) Oedema (peripheral oedema) Anorexia Tremor Enzyme inhibition
Codeine metabolism
Glucuronidation by CYP2D6 to morphine
selumetinib
Is an inhibitor of mitogen-activated protein kinases.
Trial for plexiform neurofibromas
crisaborole
It is a phosphodiesterase-4 inhibitor, mainly acting on phosphodiesterase 4B (PDE4B), which causes inflammation.[6] Chemically, crisaborole is a phenoxybenoxaborole.[6] It contains a boron atom that helps penetrate the skin and is essential for its binding activity.[8] Inhibition of PDE4B appears to suppress the release of tumor necrosis factor alpha (TNFα), interleukin-12 (IL-12), IL-23 and other cytokines, proteins believed to be involved in the immune response and inflammation.[6]
Atypical hemolytic uremic syndrome (aHUS) is caused by alternative complement pathway dysregulation, leading to systemic thrombotic microangiopathy (TMA) and severe end-organ damage. Which drug now approved and what is its mechanism of action?
eculizumab, a terminal complement inhibitor
Cotrimoxazole mechanism of action
sulfamethoxazole -> inhibits bacterial synthesis of dihydrofolic acid
trimethoprim -> blocks production of tetrahydrofolic acid
Octreotide is an analogue of
Somatostatin
Leveteracetam SE
Somnolence
Irritability
L asparginase mechanism
Breaks down asparginase which cancer cell needs to live
L asparginase SE
Allergy
Coagulopathy
Pancreatitis
Busulphan SE
Pulmonary fibrosis
Sz
VOD
Hyperpigmentation
Causes DNA cross
Inking to prevent replication
Cytarabine mechanism
Adds sugar onto nucleotide in S phase (synthesis of DNA)
Number of puffs in an inhaler
200
MgSO4 protects against CP by
Blocks NMDA receptor on glial cell preventing injury and free radicals and dilates
Cotrimoxazole works by
Inhibiting dihydrofolate
Fosfomycin targets?
Gram positive including MRSA and anaerobes
Ivacoftor is a drug for?
Modulates GSS1D potentiates molecule to surface
Kalydeco similar and is in trial phase
Dornase Alfa also called
Pulmozyme
What drug with abx neonatal sepsis reduces death
Pentoxifyline
Drug for Frederick ataxia
Idebenone (coQ10 variant)
Transenamic acid mechanism
Fibrinolytic inhibitor
Eculizumab action
Blocks C5 splitting/activation
Rituximab mechanism
Against CD20 found on B cells (triggers cell death)
Fanconi anaemia hypersensitive to what drug
Cisplatin (DNA cross linker)
Chromosome fragile
Drug for Dravet and Lennox-gastault
Dravet - stiripentol
LG - rufinamide
DRACULA SHOULD STRIP PENT HOUSE
LG FUELS THE ROOF IN A MIND
Treatment c diff mild-mod and severe
Metronidazole
IV vancomycin
What drugs delay renal clearance MTX (4)
Allopurinol
Aciclovir
Antibiotics
PPI
How does cholestyramine work and indications and side effects
Binds bile acids
High cholesterol ileum not working and itch
Side effect constipation and haemorrhoids
Diazoxide side effect? (2)
Hairy
Water retention
Phenytoin mechanism of action
Sodium channel
Erythromycin prokinetic effect mediated by
Motilin
Eculizamab inhibits?
C5 activation