FDN Exam 4: Drugs Flashcards
Antidote to opioid toxicity? What does it do?
Naloxone (Narcan)
Blocks opiod receptors
Scopolamine
Muscarinic AChR antagonist
Atropine and scopolamine are from the Belladonna plant. Used to dilate pupils. Effect is long-lasting and shorter-acting drugs are now in use
Use for motion sickness
Diisopropyl fluorophosphaste (DFP)
Organophosphate (OP)
Insecticide/nerve gas
Irreversible ACh esterase inhibitor
What does sympathomimetic mean?
producing physiological effects characteristic of the sympathetic nervous system by promoting the stimulation of sympathetic nerves
Name five muscarinic agonists
- Acetylcholine
- Methacholine
- Bethanechol
- Muscarine
- Pilocarpine
Dobutamine
Sympathomimetic
Beta1- and some alpha-adrenergic receptor agonist activity
Increases contractility, HR, and CO
Isoproterenol
Sympathomimetic
Non-selective beta-adrenergic receptor agonist
Overall increase HR, decrease in peripheral resistance, and little to no change in BP
Bethanechol
Muscarinic AChR agonist
Not metabolized
Used to increase urinary voiding
What drug is used to test for myasthina gravis?
Edrophonium
Dopamine
Sympathomimetic
Mixed action; agonist at dopamine, beta 1, alpha 1 and 2
increased contractility and HR at moderate dose, increases CO at high dose
Causes vasodilation in kidney
What two reversible ACh esterase inhibitors are used to treat Alzheimer’s disease?
Donepezil and galantamine (they both enter the CNS!)
Galantamine
Reversible ACh esterase inhibitor (weak)
Enters CNS; used for treatment of Alzheimer’s disease
Hexamethonium
Nicotinic ganglionic blocker
no CNS penetration; charged molecule
Once used as an antihypertensive but too much side effects
Methacholine
Metabolized slowly; muscarinic AChR agonist
Used as a diagnostic test for asthma. If administered and the patient is still wheezing then you know the asthma is due to a cholinergic receptor issue
Methacholine
Muscarinic agonist
Metabolized slowly; used to test bronchial reactivity/asthma - if the patient still wheezes after taking then you know a cholinergic effect is causing the asthma
What is a “quick fix” for opioid overdose?
Naloxone (Narcan) - opioid receptor antagonist
Mecamylamine
Nicotinic ganglionic blocker
Blocks CNS effects of nicotine (aka gets into the CNS)
Atropine
Muscarinic AChR antagonist
Atropine and scopolamine are from the Belladonna plant. Used to dilate pupils. Effect is long-lasting and shorter-acting drugs are now in use
Can also be used in the treatment of organophosphate poisioning (stops the slowing of the heart & CNS effects)
What drug is used to treat organophosphate posioning?
Pralidoxime (PAM)
Edrophonium
Reversible ACh esterase inhibitor
Short acting, used to test for myasthenia gravis
Muscarine
Muscarinic agonist
No clinical usage
Fab fragments treats what kind of toxicity?
Digoxin
Phenoxybenzamine
Sympatholytic
Irreversible, non-selective alpha-adrenergic receptor antagonist
Decreases upright BP & peripheral resistance
baroreceptor reflex increases HR and blood volume
What is a “quick fix” for hypoglycemia?
Dextrose
Ipratropium (Atrovent)
Muscarinic AChR antagonist
Bronchodilator
Given as an inhaled aerosol; charged molecule stays in the lung limiting systemic effects
Albuterol
Sympathomimetic
Selective beta2-adrenergic receptor agonist
Succimer treats what kind of toxicity?
Arsenic
N-acetylcysteine treats what kind of toxicity?
acetaminophen
Thiosulfate treats what kind of toxicity?
Cyanide
(note: nitrites can also be used)
Naloxone treats what kind of toxicity?
Opioid
Acetylcholine
Muscarinic AChR agonist
Rapidly metabolized
Not used clinically except with eye surgery
Antidote to digoxin toxicity? What does it do?
Fab fragments
Binds to digoxin in blood, attracting it away from cardiac receptors and enhancing excretion
Botulinum toxin
Motor nerve blocker
What two drugs treat organophosphate poisioning?
Atropine and Pralidoxime (PAM)
Where do you find nicotinic receptors?
Nicotinic Receptors are found in skeletal muscle end plates and autonomic ganglia (sympathetic and parasympathetic)
Nicotinic Receptors are ionotropic. Which means that when ACh binds to it, ions flow through it. It acts as a channel for positively charged ions, mainly sodium. Which depolarizes the cell.
Donepezil
Reversible ACh esterase inhibitor (weak)
Enters CNS; used for treatment of Alzheimer’s disease
Physostigmine
Reversible ACh esterase inhibitor/prolongs ACh in the synapse
Uncharged, enters CNS
Used for myastenia gravis, glaucoma, reversal of neuromuscular blockade after surgery, Alzheimer’s disease
Phenylephrine
Sympathomimetic
Selective alpha1-adrenergic receptor agonist
Fomepizole treats what kind of toxicity?
Methanol
(note: ethanol can also be used)
Norepinepherine
Sympathomimetic
Agonist at alpha- and beta-adrenergic receptors
Overall increases BP + peripheral resistance and decreases HR (because of baroreceptor reflex)
Which ACh esterase inhibitor(s) do not enter the CNS?
Neostigmine and Edrophonium
(note: his table doesn’t say Edrophonium doesn’t enter CNS but Google research says thats true)
Antidote to arsenic toxicity? What does it do?
Succimer
Chelator that binds to arsenic; inactivates and increases excretion
What is a “quick fix” for Wernicke’s encephalopathy?
Thiamine
Phentolamine
Sympatholytic
Reversible, non-selective alpha-adrenergic receptor antagonist
Decreases upright BP & peripheral resistance
baroreceptor reflex increases HR and blood volume
Name eight sympathomimetic drugs
- Norepinephrine
- Epinephrine
- Ephedrine
- Dopamine
- Phenylephrine
- Albuterol
- Isoproterenol
- Dobutamine
NEED PAID
What does a sympatholytic drug do? What does it commonly treat?
antagonistic to or inhibiting the transmission of nerve impulses in the sympathetic nervous system
Commonly prescribed to treat high blood pressure
Name five sympatholytic drugs
- Propranolol
- Prazosin
- Phenoxybenzamine
- Phentolamine
- Metoprolol
PPPP M
Neostigmine
Reversible ACh esterase inhibitor/prolongs the presence of ACh in the synapse
Charged, does not enter CNS
Used for myastenia gravis, glaucoma, reversal of neuromuscular blockade after surgery, Alzheimer’s disease
Antidote to methanol toxicity? What does it do?
Ethanol or fomepizole
Competitively inhibit metabolism of methanol to formaldehyde and formic acid which are responsible for severe metabolic acidosis and blindness
Three antidotes for cyanide toxicity? What does each do?
- Nitrites: Induce MetHb formation which competes with cytochrome oxidase for CN ion. Have to be careful though because excess MetHb can itself be fatal
- Thiosulfate: Increases metabolism of CN by Rhodanese, an endogenous enzyme, to thiocyanate, which is minimally toxic and readily excreted
- Hydroxycobalamin: Binds to cyanide to form cyanocobalmain, which is inactive (preferred treatment)
Propranolol
Sympatholytic
Non-selective beta-adrenergic receptor antagonist
Causes decreased HR, CO, and contractility (B1) and
increased peripheral resistance and airway resistance (B2)
Nictotine
Nicotinic AChR agonist
Where do you find muscarinic receptors?
You find Muscarinic Receptors in the brain, heart, smooth muscle, or in the Parasympathetic nervous system
When ACh binds to the muscarinic receptor, this G protein changes shape, which then allows it to phosphorylate various second messengers.
Pilocarpine
Muscarinic AChR agonist
Specificity for parasympathetic target organs
Used to stimulate salivation & to treat glaucoma (in combination with anticholinesterase)
Antidote to acetaminophen toxicity? What does it do?
N-acetylcysteine (mucomyst)
N-acetylcysteine is a Glutathoine precursor; supports intracellular glutathione pools in the liver. Glutathione conjugates and inactivates the toxic metabolite of acetaminophen
Pralidoxime (PAM)
Treatment of organophosphate (OP) poisoning (only if aging has not already occurred)
Does not cross the blood-brain barrier
Prazosin
Sympatholytic
alpha1-selective antagonist
Varenicline
Partial agonist of brain nicotine receptors associate with addiction
Ephedrine
Sympathomimetic
Mixed action
Used for asthma and as a decongestant
Metoprolol
Sympatholytic
Beta1-adrenergic receptor selective antagonist
Causes decreased HR, contractility, and CO
Epinephrine
Sympathomimetic
Agonist at alpha- and beta-adrenergic receptors
Low dose causes increased HR, decreased or no change to BP, and decreased peripheral resistance
High dose similar effects to norepinephrine
Name five reversible ACh esterase inhibitors
- Physostigmine
- Edrophonium
- Neostigmine
- Donepezil
- Galantamine
PEN DG
What is a “quick fix” for benzodiazopine toxicity?
Flumazenil (benzo antagonist)