Drug Box 3 Flashcards
Esmolol Name
Generic (Esmolol), Trade (Brevibloc)
Esmolol Classification
Cardioselective Beta Blocker/B-1 adrengeric receptor antagonist, Class II anti-arrhythmic agent
Esmolol Contraindication
Use esmolol with caution in patients with asthma; chronic obstructive pulmonary disease; atrioventricular heart block, or cardiac failure not caused by tachycardia; and diabetes
Esmolol Dose and route
SVT>loading:50 to 200 mcg/kg/min for 1 minute; follow by infusion of 50 mcg/kg/min for 4 minutes. If the desired effect is not achieved, repeat loading dose and increase infusion to 100 mcg/kg/min. May repeat the process up to a maximum of 300 mcg/kg/min. (Nagelhout handbook, pg 636)
- Loading dose: 50-300 mg/kg/min (Flood, pg 479 table)
- Single IV push- 5-10 mg (Dr. Hammons)
-10-80 mg IV (Flood, pg. 479 table)
Dosage forms:
10mg/mL in 10-mL vial for direct intravenous injection; 250 mg/mL in 10-mL ampule for intravenous infusion. Only administered IV. (Nagelhout handbook, pg 636)
Route IV
Esmolol MOA
By blocking adrengeric activity of epi and norepi, it decreases inotropic contractility, heart rate, and conduction. Esmolol increases atrioventricular refractory time decreases oxygen demand of the myocardium, and decreases atrioventricular conduction. A minor Beta 2 blockade has been reported with high IV infusion doses
Esmolol Onset
1-2 minutes
Esmolol Peak
5-6 minutes
Esmolol Duration
10-20 minutes
Labetalol Name
Trandate
Labetalol Classification
Combined α- and β-Adrenergic Receptor Antagonists
Labetalol Contraindications
bronchial asthma, 2nd-3rd degree heart block, hepatic failure
Labetalol Dose and route
Dose – IV: 0.1 - 0.5 mg/kg (Start with 5-10 mg)
Oral: 100-600 mg BID (Flood, p. 489)
5.) Route – IV, Oral
Labetalol MOA
exhibits selective α1 and non-selective β1- and β2-adrenergic antagonist effects. Presynaptic α2 receptors are spared by labetalol such that released norepinephrine can continue to inhibit further release of catecholamines via the negative feedback mechanism resulting from stimulation of α2 receptors.
Labetalol Elimination
metabolized by conjugation of glucuronic acid (enzyme that helps metabolize
drugs), with 5% of drug recovered in urine (Flood, p. 489)
Labetalol Onset
iv 1-3 min
oral 20-40 mins
Labetalol Peak
5-15min
Labetalol Duration
iv- 20mins- 2 hrs
oral- 4-12 hrs
Labetalol Misc
chronic bronchitis, emphysema, pre existing peripheral vascular disease, pheochromocytoma, and diabetes. It is contraindicated in bronchial asthma, overt heart failure, greater than first degree heart block, and hepatic failure
Metoprolol Name
Lopresor, Toprol XL
Metoprolol Classification
Beta-Blocker, Beta-1 Selective
Metoprolol Contraindication
COPD, CAD, Vulnerable to hypoglycemia
Metoprolol Dose and Route
Dose: Oral 50-400mg (Flood p. 479). Extended Release 50-150mg (Flood p.480) IV 1mg-15mg (Flood, p.479)
Route: PO or IV
Metoprolol MOA
Selective B1-Adrenergic receptor antagonist
Metoprolol Elimination
Absorbed from the gastrointestinal tract offset by sustabial hepatic first-pass-metabolism, only 40% of drug reaches systemic circulation
Metoprolol Onset
1-5 mins iv
Metoprolol Peak
iv- 20 mins
Metoprolol Duration
iv 5-7 hrs
Metoprolol Misc
Selectivity is dose related and large doses become non-selective antagonist B2 receptor as well as B1. (Flood p. 482)
Supply: 5mg/5ml or 1mg/ml
Neostigmine Name
Prostigmine
Neostigmine Classification
Anticholinesterase agent
Neostigmine Contraindications
Use with caution in patients with bradycardia, bronchial asthma, epilepsy, cardiac arrhythmias, peptic ulcer, peritonitis, or mechanical obstruction of the intestines or urinary tract
Neostigmine Dose and Route
Dose : 60 to 80 µg/kg (maximum 5mg)[dose cited from Flood, ignore other sources]
Myasthenia gravis PO 15-375 mg daily; IM 0.5-2 mg (Nagelhout Handbook P. 671)
maximum effective dose is in the 60 to 80 µg/kg range (Flood, 2016 P.335)
Dose range 25-75 mcg/kg (Nagelhout, 2018p.162)
5.) Route IV for reversal, IM or PO for myasthenia gravis (Nagelhout Handbook Page 671)
Neostigmine MOA
Mechanism of Action (MOA): It inhibits AChE by forming a drug-enzyme complex that degrades in the same manner as ACh-Cholinesterase complex, thereby increasing the concentration of endogenous ACh around the cholinoreceptors (Nagelhout hard copy textbook page 162 para 2). The ACh that accumulates at the NMJ competes with the residual molecules of NMBD for the available unoccupied nicotinic ACh receptors at the NMJ. (Flood hard copy textbook, P.334 last paragraph).
Neostigmine Elimination
Renal excretion accounts for about 50% of the excretion of neostigmine . Renal failure decreases the plasma clearance of neostigmine as much as, if not more than, that of the long-acting neuromuscular blockers
Neostigmine Onest
3-15 mins
Neostigmine Duration
0.4-4 hrs
Neostigmine Misc
Has a ceiling effect once inhibition of AChE is complete as evidenced by 4 twitches on TOF. (Flood, 2016 P.335).
May increase PONV
To minimize the muscarinic cardiovascular side effects of acetylcholinesterase inhibitors, give with glycopyrrolate (7 to 15 µg/kg) which matches the slower acting neostigmine (40 to 70 µg/kg) (Flood, 2016 P.335).
Overdose may induce a cholinergic crisis characterized by; n&v, bradycardia/tachycardia, excessive salivation, sweating, bronchospasm, weakness and paralysis. Treated by discontinuing neostigmine and administration of atropine(Flood, 2016 P.335
Robinul Name
Glycopyrrolate
Robinul Classification
Anticholinergic
Robinul Contraindication
Peptic Ulcer Disease, glaucoma, obstructive uropathy, GI disease. Mitral stenosis and cardiovascular instability in acute hemorrhage. Myasthenia gravis.
Robinul Dose and Route
4.) Dose - 10-20 mcg/kg or 0.1 - 0.2 mg (Nagelhout pg. 180, 198) (7-15 mcg/kg) - Hammon PPT
Pediatrics - 0.01 mg IV (pg. 1199, nagelhout)
5.) Route - IV, IM, inhalation - Nagelhout pg. 180,198
Robinul MOA
Synthetic quaternary ammonium compound that is an anticholinergic and blocks the effects of acetylcholines at parasympathetic sites. Reduces the rate of salivation by preventing the stimulation of acetylcholine receptors.
Robinul Elimination
feces (15%) and urine (85%) within 48 hours
Robinul Onset
Onset - 1-2 minutes IV. 15-30 minutes IM/SQ
Robinul Peak
30-45 min
Robinul Duration
2-4 hrs
Robinul Misc
- F/M Ratio of 0.13 (Value less than 1 represents incomplete transfer to fetal circulation.) Does not pass the placental barrier. Insoluble in lipids. Effective bronchodilator, but not a popular therapy of obstructive airway diseases. Mild decrease in gastric hydrogen ion secretion. Moderate relaxation of smooth muscle. Lower esophageal sphincter relaxation. Moderate antisialagogue. Moderate increase in heart rate (Less than Atropine). Less initial tachycardia than atropine; no central nervous system effects (does not pass the blood-brain barrier). Fewer systemic side effects than atropine. Onset time of glycopyrrolate and neostigmine are closely matched (used together because it is slower acting and lasts longer than atropine).
Supply: 0.2mg/ml
Zofran Name
Ondansetron
Zofran Classification
serotonin receptor 5HT3 antagonist
Zofran Contraindication
Use with caution in
o pregnant or nursing women
o Children younger than three years
o All patients with known hypersensitivity
Zofran Dose and Route
Ondansetron, 4 to 8 mg IV over 2 to 5 minutes immediately before induction (flood 697)
o Pediatric (flood 697)
§ Oral (0.15 mg/ kg)
§ IV (0.05 to 0.15 mg/kg)
§ For preadolescent children undergoing ambulatory surgery
Zofran MOA
Ondansetron is a carbazalone derivative that is structurally related to serotonin and possesses specific 5-HT3 subtype receptor antagonist properties.
Zofran Elimination
predominantly in liver e
Zofran Onset
30-60 min
Zofran Peak
1-1.5 hrs
Zofran Duration
12-24 hr
Zofran Misc
4mg/ml
Toradol Name
Sprix
Toradol Classification
NSAID
Toradol Dose and Route
Dose
IV/IM: 30 mg - 60 mg (not to exceed 120 mg/day)
Route
PO, IV, IM, intrathecal, and intranasal
Toradol MOA
Inhibits prostaglandin synthesis producine peripherally mediated analgesia
Toradol Elimination
Primarily metabolized by liver but mainly excreted from kidneys
Toradol Onset
30 mins
Toradol Peak
iv/im 1-2 hrs 2=3 hr PO
Toradol Duration
4-6 hrs
Toradol Contraindcations
Avoid giving to orthopedic patients during 1 week post-op if possible, because it can delay bone healing.
Toradol Misc
S/S: stroke, MI, GI bleeding, Stevens-Johnson Syndrome
Decadron Name
Dexamethasone sodium phosphate
Decadron Classification
long acting corticosteroid
Decadron Contraindication
Patients with peptic ulcers, osteoporosis, psychosis, psychoneurosis, acute bacterial infections, herpes zoster, herpes simplex ulceration of the eye, and other viral infections. Use it with caution in patients with DM, chronic renal failure, or infection disease in elderly patients. May increase the risk of developing TB in patients with purified protein derivative test. They may increase the risk of development of serious or fatal infection in person exposed to viral illness such as chickenpox.
Decadron Dose and Route
- Dose: Adult- Initial 0.5-9 mg IM or IV daily dependent upon the disease treated. See Nagelhout p. 625 for disease specific dosing. Children: intramuscular or intravenous push: 6 to 40mcg/kg. Must be administered slowly 3-5 minutes IV.
- Route: Oral, topical, IV, IM, IA
Decadron MOA
For PONV mechanism of action is unclear (Nagelhout p.195). Steroids inhibit the production of prostaglandins and therefore reduce pain (Nagelhout p.116)
Decadron Onset
IV/IM within 10-30 minutes, inhalation within 20 minutes (Nagelhout handbook p.625)
Decadron Peak
Peak: Oral 1-2 hours, IM ~30 to 120, IV 5 to 10 mins
Decadron Duration
Duration: Oral, topical, IV, IM, IA 36-54 hours (Flood p. 276)
Decadron Misc
Management of PONV, the mechanism of action is unclear. Chosen to treat certain types of cerebral edema (Flood, p. 694). Dexamethasone is 25 times stronger than endogenous cortisol (Flood, p.276, table 9-13). Prolongs the analgesia form interscalene blocks using ropivacaine or bupivacaine
supply: 4mg/ml
Sugammadex Name
Bridion
Sugammadex Classification
modified (gamma)y-cyclodextrin; selective neuromuscular blockade reversal agent.
Sugammadex Contraindication
renal impairment – creatinine clearance <30 ml/min (Flood p.338), allergy, bleeding;
Sugammadex Dose and Route
- ) Dose 2-16mg/kg ; for TOF(train of four) 2 then 2mg/kg, 4mg/kg for deeper block at 1-2 post tetanic count. More profound block would require range of 8-16mg/kg (Flood, pp. 338-339).
- ) Route IV over 10 seconds(Bridion pamphlet from drug rep see Dr. Hammon)
Sugammadex MOA
encapsulates/binds to steroidal neuromuscular blocking drugs (rocuronium, vecuronium, and pancuronium)
Sugammadex Elimination
mainly kidneys; approx.. 70% excreted within 6 hours, >90% within 24 hour
Sugammadex Onset
3 mins
Sugammadex Peak
with in 3 mins
Sugammadex Duration
2 hrs with normal renal function
Sugammadex Misc
Does not affect acetylcholinesterase, eliminating the need for the co-administration of an anticholinergic (Flood, pp. 337)
Does NOT work on: succinylcholine benzylisoquinolinium neuro-muslcular blockers – mivacurium, atracurium, and cisatracurium (Flood, pp.339)
If on birth control, must use non-steroidal method of contraception for at least 7 days(Nagelhout, pp.164)
Only works on rocuronium, vecuronium, and pancuronium
