- Inhibit topoisomerase II (DNA gyrase) and topoisomerase IV. - Adverse effects lower seizure threshold in patients with epilepsy tendon damage (including rupture) - the risk is increased in patients also taking steroids cartilage damage has been demonstrated in animal models and for this reason quinolones are generally avoided (but not necessarily contraindicated) in children - Lengthens QT interval Contraindications - Pregnancy - Breastfeeding - G6PD

Clinical pharmacology and Therapeutics Flashcards by SUN SHINE

Orthostatic Hypotension

Fall in SBP >20mmHg or DBP > 10mmHg within 3 minutes of standing.
Rx is Fludrocortisone or Midodrine.

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Aspirin sensitivity

Patients with aspirin sensitivity can present with either mucosal reactions (the aspirin triad of nasal polyposis, sinusitis, and asthma) or cutaneous reactions (urticaria or anaphylaxis)

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Analgesics

Partial opioid agonists (for example, buprenorphine), when used in association with morphine, may produce a reduction in the analgesic effect due to partial antagonism.

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Bicalutamide

Bicalutamide is a commonly used non-steroidal, anti-androgen therapy. It works by blocking the androgen receptors and is typically used together with a gonadotropin-releasing hormone (GnRH) analogue or orchidectomy in the management of advanced prostate

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Metastatic Hormonal therapy

1- GnRH agonists: e.g. Goserelin (Zoladex.
2- GnRH antagonists such as degarelix
3- bicalutamide
non-steroidal anti-androgen
blocks the androgen receptor
4- cyproterone acetate
steroidal anti-androgen
prevents DHT binding from intracytoplasmic protein complexes
5- abiraterone
androgen synthesis inhibitor.
6- bilateral orchidectomy
7- Chemotherapy with docetaxel

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Ondansetron

Ondansetron is a 5-HT 3 serotonin antagonist
-Adverse effects
prolonged QT interval
constipation is common

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Live attenuated Vaccines

BCG
measles, mumps, rubella (MMR)
influenza (intranasal)
oral rotavirus
oral polio
yellow fever
oral typhoid

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Alcohol withdrawal

Alcohol withdrawal
symptoms: 6-12 hours
seizures: 36 hours
delirium tremens: 72 hours

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ADRENALINE

Adrenaline induces hyperglycemia, hyperlactatemia and hypokalaemia.

-Adrenaline is a sympathomimetic amine with both alpha and beta adrenergic stimulating properties

Indications
- anaphylaxis
- cardiac arrest

Recommend Adult Life Support (ALS) adrenaline doses
anaphylaxis: 0.5ml 1:1,000 IM
cardiac arrest: 10ml 1:10,000 IV or 1ml of 1:1000 IV

Management of accidental injection e.g., resulting in digital ischaemia
local infiltration of phentolamine.

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Quinolones

Inhibit topoisomerase II (DNA gyrase) and topoisomerase IV.
Adverse effects
lower seizure threshold in patients with epilepsy
tendon damage (including rupture) - the risk is increased in patients also taking steroids
cartilage damage has been demonstrated in animal models and for this reason quinolones are generally avoided (but not necessarily contraindicated) in children
Lengthens QT interval

Contraindications
- Pregnancy
- Breastfeeding
- G6PD

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Dipyridamole

Dipyridamole is a non-specific phosphodiesterase inhibitor and decreases cellular uptake of adenosine.

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Aspirin

Aspirin causes irreversible inhibition of the COX-1 and COX-2 enzymes which blocks the formation of thromboxane A2 in platelets. This reduces platelet aggregation.

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Mercury poisoning

Features
- paraesthesia
- visual field defects
- hearing loss
- irritability
- renal tubular acidosis

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P450 Enzyme system

Inducers of the P450 system include
antiepileptics: phenytoin, carbamazepine
barbiturates: phenobarbitone
rifampicin
St John’s Wort
chronic alcohol intake
griseofulvin
smoking (affects CYP1A2, reason why smokers require more aminophylline)

Inhibitors of the P450 system include
antibiotics: ciprofloxacin, erythromycin
isoniazid
cimetidine,omeprazole
amiodarone
allopurinol
imidazoles: ketoconazole, fluconazole
SSRIs: fluoxetine, sertraline
ritonavir
sodium valproate
acute alcohol intake
quinupristin

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G6PD Deficiency

Ciprofloxacin is contraindicated in G6PD deficiency

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Quinine toxicity (cinchonism)

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Quinine toxicity (cinchonism) presents with myriad
- ECG changes ( Prolong QRS and QT interval),
- hypotension
- metabolic acidosis
- hypoglycaemia
- tinnitus
- flushing and visual disturbances.
- Flash pulmonary oedema

Tricyclic overdose

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Widened QRS or arrhythmia in tricyclic overdose - give IV bicarbonate

IL-8

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IL-8 - main functions include: neutrophil chemotaxis

Ciclosporin + Tacrolimus

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Ciclosporin + tacrolimus: inhibit calcineurin thus decreasing IL-2

Mycophenolate mofetil

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Mycophenolate mofetil inhibits inosine monophosphate dehydrogenase.

Methotrexate

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Methotrexate is an antimetabolite which inhibits dihydrofolate reductase

Lead poisoning

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Abdominal pain, constipation, neuropsychiatric features, basophilic stippling → lead poisoning.

Management of Lead poisoning

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Dimercaptosuccinic acid (DMSA)
D-penicillamine
EDTA
Dimercapro

MMDA

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MDMA (Ecstasy) poisoning is associated with hyponatraemia

Moxonidine

Moxonidine is a centrally acting antihypertensive drug, which works by stimulating imidazoline receptors in the brain. This stimulation results in reduced sympathetic outflow from the central nervous system, leading to decreased vascular resistance and lower blood pressure. It's mainly used for treating essential hypertension.

Centrally acting Antihypertensives

1- Methyldopa: used in the management of hypertension during pregnancy 2- Moxonidine: used in the management of essential hypertension when conventional antihypertensives have failed to control blood pressure 3- Clonidine: the antihypertensive effect is mediated through stimulating alpha-2 adrenoceptors in the vasomotor centre

Foods with high Glycaemic index

Foods with a high glycaemic index (GI), such as white bread, causes a rapid spike in blood glucose levels, followed by a quick drop

Drugs affected by acetylator status

Drugs affected by acetylator status - Isoniazid - Procainamide - Hydralazine - Dapsone - Sulfasalazine

Drugs exhibiting zero-order kinetics

Drugs exhibiting zero-order kinetics - Phenytoin - Salicylates (e.g. high-dose aspirin) - Heparin - Ethanol

Phase I reactions

Phase I reactions: oxidation, reduction, hydrolysis.

Phase 2 Reactions

Phase 2 reactions: Conjugation.

Minimal glucocorticoid activity, very high mineralocorticoid activity,

Fludrocortisone

Very high glucocorticoid activity, minimal mineralocorticoid activity

Dexamethasone Betamethasone

Raburicase

Rasburicase - a recombinant version of urate oxidase, an enzyme that metabolizes uric acid to allantoin

Laboratory Tumor lysis syndrome

Uric acid > 475umol/l or 25% increase potassium > 6 mmol/l or 25% increase phosphate > 1.125mmol/l or 25% increase calcium < 1.75mmol/l or 25% decrease

Clinical Tumor Lysis syndrome

- Increased serum creatinine (1.5 times upper limit of normal) - cardiac arrhythmia or sudden death - seizure

Lidocaine

Local anesthetic toxicity can be treated with IV 20% lipid emulsion

Clinical pharmacology and Therapeutics Flashcards

(37 cards)