Pre-op meds - test 1 Flashcards
Histamines are endogenous substances that are released from ___________ and _______________.
Basophils; Mast Cells
What does histamine do to the airway?
Contraction of smooth muscles in the airway.
What does histamine do in the stomach?
Acid Secretions in the stomach.
Histamine causes what NTs to be released in the CNS?
Histamine will cause the release of serotonin, acetylcholine, and norepinephrine in the CNS.
What drugs will induce histamine release?
Morphine, Protamine, Mivacurium, Atracurium
When H1 histamine receptors are activated it can activate ______, _________, __________, and ________ receptors.
Muscarinic, Cholinergic, 5HT3, Alpha-adrenergic
When H2 histamine receptors are activated, it can activate ________ and ________ receptors.
5HT3, Beta-1
When histamine binds to an H1-receptor what will be the result?
Hyperalgesia and inflammatory pain (insect sting)
Allergic rhino-conjunctivitis symptoms
When histamine binds to an H2-receptor what will be the result?
Elevate cAMP (Beta1-like stimulation, tachycardia)
Increase acid and volume production
Activation of both H1 and H2 receptors will result in what symptoms?
Prostacyclin Release, Capillary permeability, Tachycardia, Hypotension d/t release of NO, Flushing
What is the most accurate description of an antihistamine?
Inverse Agonist
They don’t prevent the release of histamine but responses
What are the effects of H1 receptor antagonists on the following areas? Vestibular System, Airway Smooth Muscle, Cardiac Endothelial:
Vestibular System: Effective for motion sickness
Airway Smooth Muscle: protection against bronchospasms
Cardiac Endothelial: provide cardiac stability
The first-generation H1 antagonist causes a lot of ____________ as a side effect.
sedation
Can you develop tachyphylaxis from H1 receptors?
No
What are the side effects of H1 receptor antagonists?
Blurred Vision, Urinary Retention, Dry Mouth, Drowsiness/Sedation (first gen)
What are examples of H1 receptor antagonist drugs?
Diphenhydramine (Benadryl), Promethazine (Phenergan), Cetirizine (Zyrtec), Loratadine (Claritin)
This H1 receptor drug is mostly used as an antipruritic and pre-treat procedure-related allergy (IVP dye)
Benadryl
Diphenhydramine inhibits the afferent arc of the ________________.
Oculo-emetic reflex
Diphenhydramine can stimulate ventilation by augmenting the relationship of ____________ and ___________ drive.
Hypoxic, Hypercarbic
Only if given as a solo administration
What is the IV dose of Benadryl?
25-50mg IV
What is the half-time of Benadryl?
7-12 hours
Which H1 receptor antagonist is a great anti-emetic and is used as a rescue and reduces peripheral pain levels (anti-inflammatory effects).
Promethazine
What is the IV dose of Promethazine?
12.5-25mg IV (give less to the elderly)
How long does it take to onset for Promethazine?
5 minutes for onset
What is the half-time of Promethazine?
9-16 hours
What were the black box warnings for Phenergan?
Can cause death in children under the age of 2.
Can cause extravasation and ischemia to the tissue from IV injection.
H2 receptors antagonist are most commonly used in __________.
Duodenal ulcer disease / GERD
How does an H2 receptor antagonist work?
Decrease hypersecretion of gastric fluid (H+) from gastric parietal cells and decrease cAMP, which will decrease gastric volume and increase pH.
H2 receptor antagonist can increase serum creatine by _______% d/t competition for tubular secretion.
15%
What are the side effects of H2 receptor antagonists?
HA/Confusion (Elderly), Bradycardia, Diarrhea, Skeletal Muscle Pain, Weakened Gastric Mucosa, Creatine Increase
Overgrowth of ____________ can increase pulmonary infections d/t weakened gastric mucosa from prolonged administration of H2 antagonist.
Candida Albicans
What are examples of H2 receptor antagonists?
Cimetidine (Tagamet), Ranitidine (Zantac), Famotidine (Pepcid)
How is Cimetidine metabolized?
CYP450, hepatic metabolism, renal clearance
Cimetidine strongly inhibits CYP 450 and can affect the metabolism of which drugs?
Warfarin, Phenytoin, Lidocaine, Tricyclics, Propranolol (Inderal), Nifedipine, MEperidine, Diazepam
What are the adverse effects of Cimetidine?
Bradycardia, Hypotension (rapid infusion), Increase Prolactin, Impotence (Inhibits dihydrotestosterone binding to androgen receptors)
What is the dose of cimetidine?
150-300mg IV
What is the renal dosing for cimetidine?
75-150mg IV
How is Ranitidine metabolized?
CYP450, hepatic metabolism, renal clearance
What is the dose of Ranitidine?
50mg diluted to 20cc given over 2 minutes.
What is the renal dosing for Ranitidine?
25mg diluted to 20cc given over 2 minutes.
How is Famotidine metabolized?
CYP450, hepatic metabolism, renal clearance
What interference is Famotidine involved with?
Interferes with phosphate absorption and can result in phosphatemia.
Bone fractures or hips hurting
What is the dosing for famotidine?
20mg IV
What is the renal dosing for famotidine?
10mg IV
What is the half-time for famotidine?
2.5-4 hours (most potent and longest of all H2 receptor antagonist)
What group of drugs irreversibly bind to acid secretion pumps and inhibit the movement of protons (H+) across the gastric parietal cells?
Proton Pump Inhibitors
How many days does it take for the onset of PPIs?
3 to 5 days
What are PPIs most effective against?
Controlling gastric acidity, Decreasing Volume
PPIs are more effective than H2 receptors in what 4 areas?
Healing esophagitis, Healing ulcers, Relieving symptoms of GERD, Best treatment of Zollinger-Ellison Syndrome
What are examples of PPI?
Omeprazole (Prilosec), Pantoprazole (Protonix), Lansoprazole (Prevacid), Dexlansoprazole (Dexilent)
What have PPIs been associated with?
Bone Fractures, SLE, Acute Intestinal Nephritis, C-diff, Vitamin B12, Magnesium Deficiency
PPI will inhibit ____________ metabolism.
Warfarin (Warfarin can work too well with PPI, watch the INR)
Clopidogrel (Clopidogrel won’t work as well with PPI)
Omeprazole is enteric coated and is a prodrug that protonates in the _____________ to its active form.
Parietal Cells
Omeprazole only inhibit pumps that are present, acid inhibition increases with repeated dosing, but it only covers about ____% maximum inhibition.
66%
How is omeprazole metabolized?
CYP metabolism
What is the dosing of omeprazole?
If given PO, how long before surgery?
40mg in 100cc NS given over 30 minutes
PO- at least 3 hours prior to surgery
What are the side effects of omeprazole?
HA (crosses BBB), Agitation (crosses BBB), Confusion (crosses BBB), Abdominal Pain, N/V, Flatulence, SB bacterial overgrowth
How is Protonix metabolized?
CYP metabolism
Protonix has a greater ____ and longer ____ compared to omeprazole.
Greater bioavailability and greater half time
What is the dose of Protonix?
40mg in 100cc given over 2-15 minutes
How long before surgery can you give protonix?
1 hour before surgery to decrease gastric volume and increase pH (works as fast as ranitidine)
PPI’s are the treatment of choice for ______, _______, and _______.
GERD, Gastroduodenal Ulcers, Acute upper GI Hemorrhage (post EGD treatment)
What is given to treat NSAID ulceration?
Omeprazole
What will protect the acidity of aspiration pneumonitis and be the most cost-effective for intermittent symptoms?
H2 antagonist
What is a particulate antacid?
Particulate antacids are Aluminum or Magnesium based. Aspiration equals acid aspiration.
What is a non-particulate antacid?
Non-Particulate antacids are Sodium, Carbonate, Citrate, or Bicarb base. Neutralize Acid.
What are long-term effects of all antacids?
If pH is too high, acid breakdown of food will be inhibited and acid rebound can occur.
What are the long-term effects of magnesium-based antacids?
Magnesium-based: Osmotic diarrhea, neurological/neuromuscular impairment
What are the long-term effects of calcium-based antacids?
Calcium-based: Hypercalcemia, Kidney stones
What are the long-term effects of sodium-based antacids?
Sodium-based: Hypertension
How does sodium citrate (Bicitra) neutralizes acid?
The Bicitra and acid are combined to make salt, CO2, and water, resulting in neutralization.
Sodium citrate increases __________.
Intra-gastric volume
What is the dose of sodium citrate?
15-30 mL
When does sodium citrate lose its effectiveness?
After 30-60 minutes
Pregnancies are considered full stomach after _________ weeks.
12 weeks
What types of drugs are known for stimulating gastric motility (prokinetic)?
Dopamine-blocking drugs for full stomachs.
What do prokinetic drugs increase?
Lower Esophageal Sphincter tone.
What do prokinetic drugs stimulate?
Peristalsis.
What do prokinetic drugs relax?
Pylorus and Duodenum.
Who is contraindicated by dopamine blockers?
Individuals who are dopamine depleted (Parkinson’s).
What are the side effects of dopamine blockers?
Extrapyramidal reactions (easily crosses BBB), Orthostatic Hypotension, can affect the chemoreceptor trigger zone, no change in gastric pH.
What are examples of dopamine blockers?
Metoclopramide (Reglan), Domperidone (not available in the US), Droperidol (Inapsine).
What is the FDA-cleared drug for diabetic gastroparesis?
Metoclopramide (Reglan).
What are the side effects of Reglan?
Abdominal cramps from rapid infusion, Muscle Spasm, Hypotension, Sedation, Increase Prolactin Release, Neuroleptic malignant syndrome, Decrease plasma cholinesterase levels.
What is the dose of Reglan?
When do you give reglan before induction?
10-20mg given over 3 to 5 minutes.
15 to 30 minutes before induction
Unlike Reglan, what drug does not cross the BBB and has no anticholinergic activity?
Domperidone.
What does Domperidone increase secretion of?
Prolactin.
Why is Domperidone not FDA-approved?
Due to Dysrhythmias and Sudden Death.
What drug was initially developed for schizophrenia and psychosis?
Droperidol (Inapsine).
What adverse side effects can Droperidol cause?
Extrapyramidal syndrome and Neuroleptic Malignant Syndrome.
What CNS depressants should be avoided with Droperidol?
Barbiturates, Opioids, General Anesthesia.
Droperidol is more effective than what for N/V?
Reglan.
Droperidol is equally effective to how much of Zofran for N/V?
4 mg of Zofran.
What is the black box warning for Droperidol?
Prolonged QT intervals, Torsades with higher doses, Serious Drug Interactions (amio, diuretics, beta blockers, CCB, steroids)
What is the dose for Droperidol?
0.625 to 1.25mg IV.
____________ is released from the chromaffin cells of the small intestine and stimulates ____________ through 5HT3 receptors that cause __________.
Serotonin
Vagal afferents
Vomiting
Where is a large concentration of 5HT3 receptors?
Brain and GI Tract.
What group of drugs is now used for PONV?
5HT3 antagonist.
Competitive antagonist with almost no side effects
What is 5HT3 not effective against?
Motion sickness and vestibular stimulation.
What are examples of 5HT3 antagonists?
Ondansetron (Zofran), Granisetron (Kytril), Dolasetron (Anzemet).
Which drug is the first 5HT3 antagonist and does not cross the BBB?
Ondansetron (Zofran).
What are the side effects of Zofran?
HA, Diarrhea, Slight QT prolongation.
What is the dose of Zofran?
What is the plasma half-life?
4 or 8mg IV.
4 hours (give zofran at the end of the case)
What group of drugs centrally inhibits prostaglandin synthesis and control endorphin release?
Corticosteroids.
also has an anti-inflammatory effect resulting in less post-op pain, and less opioid use
What is the diabetic risk of Decadron?
Perioperative Hyperglycemia (minimal side effect with one dose)
What is another side effect of Decadron?
Perineal Burning/Itching (rapid IV push)
What is the dose of Decadron?
4mg or 8mg.
What is the delay in onset for Decadron?
2 hours.
Give at the beginning of the case
How long does the efficacy of Decadron persist?
24 hours.
When will you consider giving an increased dose of Decadron?
Airway trauma d/t multiple intubation attempts. (12 or 16 mg)
What are Scopolamine patches used for?
They are muscarinic antagonists (anticholinergic) for nausea and vomiting.
they have both central and peripheral effects (crossess the BBB - sedation)
What are the side effects of Scopolamine patches?
Dilated pupils, Sedation.
What are the peak concentration hours for Scopolamine patches?
8 to 24 hours.
How long does it take the Scopolamine patch to work?
4 hours for onset of action.
What is the priming dose of Scopolamine?
140 mcg.
How much scopolamine will be given over the next 72 hours?
1.5mg.
Where will the Scopolamine patch be placed?
Post-auricular.
What group of drugs stimulates G-proteins and relaxes smooth muscles in the airway?
Beta-receptor agonists (Bronchodilators).
Bronchodilators can reduce inflammatory cell activation, directly relax smooth muscles, and increase FEV1 by _________% within _____ minutes (2 puffs).
15% improvement in 6 minutes.
How do you deliver an inhaled SABA?
Discharge inhaler while taking a slow deep breath over 5-6 seconds
What percentage of the inhaled SABA reaches the lungs?
12%.
What percentage of the inhaled SABA is delivered to the lungs through mechanical ventilation?
50-70%.
How often are inhaled SABAs given?
Every 4 hours.
What are the side effects of beta agonists?
Tremor, Tachycardia, Transient Decrease in arterial oxygenation, Hyperglycemia.
What are examples of bronchodilators?
Albuterol (Proventil), Levo-albuterol (Xopenex).
What are ways to deliver SABA?
Inhaler, Puff piece nebulizer, Syringe.