Drugs and their antidotes (toxicology) Flashcards
Opioid
Naloxone (Narcan), Nalmefene (Revex), Naltrexon (Revia)
MoA: Naloxone is an opioid antagonist. It competes at three CNS opioid receptors (μ, κ, δ) and leads to reversal of the depressive opioid effects.
IV is best in emergency, rapid onset of action (1-2 minutes.
Because is has no agonist activity, naloxone will not worsen respiratory depression. When administered, patient should be monitored for respiratory rate changes (and opiate withdrawal symptoms) as the goal of therapy is to restore adequate spontaneous respirations. to avoid withdrawal, use the lowest possible dose that maintains proper ventilation.
Patient should be observed for RD after discontinuation of therapy because the half-life of naloxone may be shorter than that of the opioid. If patient is unresponsive to 10mg naloxone, it is doubtful that an opioid is causing the RD.
Use with caution in the physically dependent (can precipitate withdrawal) and those with preexisting cardiovascular disease or those receiving cardiotoxic drugs.
Digoxin, Digitoxin
Digoxin immune antibody fragment or Digoxin immune Fab (Digibind, DigiFab)
MoA: Binds digoxin in plasma, promotes redistribution from tissues, and enhances elimination in the urine. Digoxin becomes inactive once bound to Digoxin immune Fab.
Chronic digoxin toxicity typically begins with the nausea/vomiting/diarrhea/fatigue/confusion/blurred vision or diplopia/arrhythmias. Toxicity can be cause by deterioration of renal function, hypokalaemia, or drug interaction.
Acute digoxin toxicity has early symptoms similar to those of chronic but the onset is more abrupt.
Digoxin immune Fab is a monovalent, digoxin-specific, antigen-binding fragment (Fab) that is produced in healthy sleep. Random fact, it should not be used in patients hypersensitive to sheep because Digoxin immune Fab is derived from the antibodies of sheep.
Cyclophosphamide, Ifosfamide
Mesna (Mesnex)
Coumadin/Warfarin/Superwarfarins
Vitamin K1 (Mephyton, AquaMephyton), Fresh frozen plasma
Heparin
Protamine sulfate
Iron
Deferoxamine (Desferal)
Arsenic, Gold, Lead
Dimercaprol aka British antilewisite (BAL-in-Oil), Succimer (Chemet)
Cyanide
Sodium nitrite 3% + Sodium thiosulfate (Cyanide Antidote Kit), Hydroxocobalamin (Cyanokit)
Benzodiazepine
Flumazenil (Romazicon)
MoA: It’s a competitive antagonist of the benzodiazepine receptor in the central nervous system.
In suicidal overdose, flumenazil is rarely used because of the risk of potential co-ingestants. It should not be used in other mixed overdoses that can decrease the seizure threshold (i.e. haloperidol, bupropion, lithium). Co-ingestants of tricyclic antidepressants may precipitate ventricular dysrhythmias or seizures.
Atropine, Anticholinergic compounds
Physostigmine salicylate (Antilirium)
Acetaminophen
Acetylcysteine (Mucomyst 10%/20%, Acetadote 20%)
MoA: supplies glutathione to aid metabolsim of the reactive metabolite. May provide sulfate for acetaminophen metabolism and minimize the formation of free radicals.
For best results, administer <10 hours after overdose. Minimally effective 24 hours after ingestion.
Therapy is determined by obtaining a serum concentration of acetaminophen between 4-24 hours after ingestion and plotting it on the acetaminophen nomogram to determine whether there is a risk for hepatotoxicity.
Doxorubicin
Dexrazoxane (Zinecard)
Anticholinesterase-Organophosphates insecticide poisoning or chem-bioterrorism nerve agent poisoning
Pralidoxime hcl (Protopam) [with Atropine]
MoA: Pralidoxime is indicated in combination with atropine (to resolve nicotinic [muscle weakness, diaphragmatic weakness, fasciculations, muscle cramps] and central [coma, seizures] cholinergic manifestations).
It is ineffective for organophosphates without anticholinesterase activity! Use in carbamate poisoning is controversial but some sources recommend it in severe cases.
Insulin, β-blocker, CCB
Glucagon (GlucaGen), IV Dextrose
also Calcium chloride 10% for CCB
Digitalis toxicity, hypercalcaemia
Edetate disodium
Lead
Succimer (Chemet), Dimercaprol aka British antilewisite (BAL-in-Oil) Edetate calcium disodium - EDTA (Calcium Disodium Versenate)
Acetylcholine, Cholinergic agent, Carbamates, Organophosphates, (Bradycardia)
Atropine
MoA: It’s an anticholinergic agent that competitively inhibits acetylcholine at muscarinic receptors. Little to no effect on nicotinic receptors.
Dosaging varies, but in severe poisoning doses of up to 100mg over a few hours or several weeks may be required.
When large doses of atropine are used, the product should be preservative-free because agents such as benzyl alcohol or chlorobutanol can produce their own toxicity.
Cyanide
Hydroxocobalamin
Methotrexate, Trimethorpim, Pyrimethamine
LeucovorinCa2+ (Wellcovorin)
Ethylene glycol, methanol
Ethanol 10%, Fomepizole (Antizol)
Isoniazid
Vitamin B6 - Pyridoxine
Methemoglobinaemia
Methylene blue