Reversal Associated Dosages Flashcards
Narcan (alternate name):
Naloxone
Narcan structure:
Derivative of Oxymorphone
Narcan MOA:
Competitive agonist of all opioid receptors
Greatest for Mu
Narcan Onset:
1-2 min
Narcan Duration of action:
30-60 min
Narcan PB:
50%
Narcan Metabolism:
Hepatic, Renal
Narcan IV adult Dose:
IV Adult: 0.4 - 2 mg
(repeat as needed)
Narcan IV peds Dose:
IV peds: 0.1 mg/kg (max 2mg)
(repeat as needed)
Narcan Side effects:
- Reversal of opioids
- increased resp drive
- increased BP
- N/V
- Arrythmias
Narcan Contraindications / cautions:
- Pulmonary edema
- Sudden death
- May need to re-dose
- Do not give fast
5.
Sugammadex (alternate name):
Bridion
Sugammadex Structure:
Gamma cyclodextrin (selective relaxant-binding agent)
Sugammadex MOA:
- Hydrophobic cavity
- Encapsulates the steroid NMB (specifically roc)
- Forms a complex that cannot have an effect on receptors or acetylcholinesterase
- Highly water soluble
Sugammadex Onset:
1-2 min
Sugammadex duration of action:
2-16 h
Sugammadex PB:
0%
Sugammadex Metabolism:
Really excreted unchanged (80%)
Sugammadex IV dose:
IV: 2 mg/kg (TOF 2-4)
IV: 4 mg/kg (TOF 0-1)
IV: 16 mg/kg (1.2 mg/kg RSI reversal)
Sugammadex side effects:
- Bradycardia
- Nausea
- Headache
- Hepatic stable
- Potential asystole
Sugammadex Contraindications / cautions
- Birth control pills ineffective for 1 week
- Caution in renal disease
- Known hypersensitivity
- If need to reintubate, use a different NMB
- Ensure adequate reversal before extubation: head lift 5 secs, spontaneous ventilation, eye opening, hand grip, cough/gag reflex, leg raise
Glycopyrrolate (alternate name):
Robinul
Glycopyrrolate structure:
Anticholinergic
Quaternary ammonium
Glycopyrrolate MOA:
- Block muscarinic receptors
- Not nicotinic so that NMB can be antagonized while muscarinic effects are minimized
- blocks parasympathetic effects
Glycopyrrolate Onset:
1-2 min
Glycopyrrolate duration of action:
2-4 h
Glycopyrrolate PB:
30%
Glycopyrrolate metabolism:
Limited hepatic, 80% unchanged renally
Glycopyrrolate IV dose:
0.6-1 mg (equal volume to anticholinesterase)
0.1-0.2 mg (antisalagouge, effect 2-4 x atropine)
Glycopyrrolate side effects (same as other anticholinergics):
- Bronchodilation
- Decrease PONV
- Dry mouth
- Pupil dilation
- Increase HR
Glycopyrrolate Contraindications / cautions:
- Give prior to anticholinesterase
- Adjust dose if already tachycardic
- Mix with equal volume of anticholinesterase
- Tachycardia may be seen when administered with pyridostigmine b/c of its slow onset
- Does not cross BBB
- Overdose: mad as a hatter (confusion), blind as a bat (mydriasis), hot as a hare (no sweating), dry as a bone (dry mouth), red as a beet (flushing), full as a flask (urinary retention) (can’t see, pee, spit, or shit)
Atropine (alternate name):
Atropen
Atropine structure:
Anticholinergic
Tertiary amine
Atropine MOA:
- Competitively bind to the Ach receptor
- prevents cGMP or cAMP mediated effects
Atropine Onset:
1-2 min
Atropine duration of action:
1-2 h
Atropine PB:
30%
Atropine Metabolism:
Liver 50%, renal 50% unchanged
Atropine IV dose:
IV: 15 mcg/kg (with equal volume anticholineasterase) or
IV: 1-2 mg (with equal volume anti cholinesterase)
(HR effects 2-4 x glycopyrrolate)
Atropine side effects (same as other anticholinergics):
- Bronchodilation
- Decrease PONV
- Dry mouth
- Pupil dilation
- Increase HR
Atropine Contraindications / cautions:
- Crosses BBB
- Decreased baroreceptor sensitivity
- High variability in HR
- Does not increase HR in Heart transplant patients
- Overdose: mad as a hatter (confusion), blind as a bat (mydriasis), hot as a hare (no sweating), dry as a bone (dry mouth), red as a beet (flushing), full as a flask (urinary retention) (can’t see, pee, spit, or shit)
Scopolamine (alternate name):
Hyoscine
Scopolamine structure:
Anticholinergic
Tertiary amine
Aromatic ester
Scopolamine MOA:
Competitive antagonist of peripheral and central muscarinic receptors
Scopolamine Onset:
4 h
Scopolamine duration of action:
3 days
Scopolamine PB:
30%
Scopolamine Metabolism:
CYP3A4, then conjugated and excreted by the kidneys
Scopolamine transdermal dose:
1.5 mg patch
Releases 0.5 mg/day
Stays on for 3 days
Scopolamine side effects (same as other anticholinergics):
- Bronchodilation
- Decreases PONV
- Dry mouth
- Pupil dilation
- Increases HR
Scopolamine Contraindications / cautions:
- Delirium
- Sedation
- Constipation
- Blurred vision
- Dizziness
- Crosses BBB
- Avoid in narrow-angle glaucoma (increases eye pressure)
- Overdose: mad as a hatter (confusion), blind as a bat (mydriasis), hot as a hare (no sweating), dry as a bone (dry mouth), red as a beet (flushing), full as a flask (urinary retention) (can’t see, pee, spit, or shit)
Neostigmine (alternate name):
Bloxiverz
Neostigmine structure:
Anticholinesterase
Quaternary Ammonia
Neostigmine MOA:
- Inhibits acetylcholinesterase at NMJ
- Increase Ach at the NMJ
- Ach competes with NMB
- reversal of nondepolarizing NMB
Neostigmine Onset:
5-15 min
Neostigmine duration of action:
1-2 h
Neostigmine PB
30%
Neostigmine Metabolism:
Hepatically & plasma esterase, Renally excreted
Neostigmine IV dose:
IV: 0.05-0.07 mg/kg
MAX DOSE: 5 mg
Ceiling effect at 0.07 mg/kg
Neostigmine side effects:
- Cholinergic Crisis (DUMBELLS)
- Diarrhea
- Urination
- Miosis
- Bradycardia
- Emesis
- Lacrimation (tears)
- Lethargy
- Salivation
Neostigmine Cautions / contraindications
- Always mix with anticholinergic
- Must have 1-2 twitches on TOF
- Previous allergic rxn
- Use caution in pt with asthma
- Does not cross the BBB
Physostigmine (alternate name):
antilirium
Physostigmine structure
Anticholinesterase
Tertiary amine
Physostigmine MOA:
Inhibits acetylcholinesterase, thus allowing acetylcholine to increase at the NMJ
Physostigmine Onset:
5-10 min
Physostigmine duration of action:
30-60 min
Physostigmine PB:
30%
Physostigmine Metabolism:
Hepatically & plasma esterase, Renally excreted
Physostigmine IV dose:
IV: 15-60 mcg/kg
Physostigmine side effects:
- Cholinergic Crisis (DUMBELLS)
- Diarrhea
- Urination
- Miosis
- Bradycardia
- Emesis
- Lacrimation (tears)
- Lethargy
- Salivation
Physostigmine Contraindications / cautions:
- Used in central anticholinergic syndrome
- Used for reversal of confusion following atropine/ scopolamine
- Crosses BBB
- Allergic reaction
Pyridostigmine (alternate name):
Mestinone
Pyridostigmine structure:
Anticholinesterase
Quaternary ammonia
Pyridostigmine MOA:
- Inhibit acetylcholinesterase at the NMJ
- Allows for increased Ach at the NMJ to compete with NMB
- results in the reversal of competitive nondepolarizing NMB
Pyridostigmine Onset:
10-20 min
Pyridostigmine duration of action:
1-2 h
Pyridostigmine PB:
30%
Pyridostigmine Metabolism:
Limited hepatic metabolism,
80% unchanged Renal
Pyridostigmine IV dose:
IV: 0.1 - 0.3 mg/kg
Pyridostigmine side effects:
- Cholinergic Crisis (DUMBELLS)
- Diarrhea
- Urination
- Miosis
- Bradycardia
- Emesis
- Lacrimation (tears)
- Lethargy
- Salivation
Pyridostigmine Contraindications / cautions:
- Always mix with anticholinergic
- Must have 1-2 twitches on TOF
- Previous allergic rxn
- Use caution in pt with asthma
- Does not cross the BBB
Flumazenil alternate name:
Romazicon
Flumazenil structure:
1, 4 imidazobenzodiazepine derivative
Flumazenil MOA:
Competitive benzodiazepine antagonist with high receptor affinity
Flumazenil Onset:
1-2 min
Flumazenil Duration of action:
30-60 min
Flumazenil PB:
50%
Flumazenil Metabolism:
Hepatic to inactive metabolites
Flumazenil IV dose:
- IV Initial dose: 0.2 mg
- IV Repeat dose: 0.3-0.5 mg Q 60 seconds (max 3 mg)
- > 5 mg w/o response = alternate reason for sedation
Flumazenil side effects:
- Benzodiazepine reversal
- Seizure
- Nausea & Vomiting
- Tachycardia
- Hypertension
Flumazenil Contraindications / Cautions
- Allergic Reaction
- Arrhythmias
- Withdrawal Symptoms
- Dizziness/Lightheadedness
- CAUTION: avoid with seizure patients on antiepileptics