Pharm test 2 Flashcards
Efficacy
Maximal response a drug can produce
Potency
Measure of dose required to produce a response
Name strong opioid agonist (high efficacy)
Morphine, methadone, Fentanyl, oxycodone, and heroin
Name partial agonists for opioid
Codeine, hydrocodone, tramadol, tapentadol
Opioids that also have antidepressant
Tramadol and tapentadol
What would you use to treat a opioid addiction as an alternative to methadone
Buprenorphine (partial mu agonist, kappa opioid antagonist) -compete with heroin, so can’t get high because buprenorphine higher affinity -must give sublingual, because inactive if given orally -slow acting
A patient comes in with an opioid overdose what do you use to treat them?
Naloxone ( not orally active ) Antagonist with high affinity, no efficacy
A patient is struggling with alcohol dependence and comes to you for help. What drug can you give them to help?
Naltrexone (Is orally active) Antagonist with high affinity, no efficacy
How does morphine and other related opioids work? Side effects?
Activate the mu opioid receptor Side affects: constipation, respiratory depression, analgesia, sedation
Tolerance of opioids causes want?
Increase dose required to produce desired therapeutic effects
Physical dependence of opioids withdrawl signs?
Muscle aches, insomnia, rhinorrhea, your name, piloerection
Hyperalgesia opiods
Can happen when go off opioids Sensitization of pronociceptive pathways
Heroin pharmakinetics
Opioids: Rapid onset blood brain barrier, short duration ( more hydrophobic form)
Methadone, oral pharmakinetics
Opioids: Slowly absorbed, slowly penetrate. Slowly cleared, so drug accumulation can occur more easily and lead to toxicity. Hard to up titrate
Naloxone, oral pharmakinetics
Prevent abuse of drugs when combine with other drug. Opioids: Rapid metabolized, give with buprenorphine or oxycodone to prevent diversion Can put inside drug so get withdrawl effects if inject (abuse deterrent)
Loperamide, oral pharmakinetics
Opioids: Doesn’t penetrate brain, anti diarrheal ( reduce gut motility)
18-year-old woman with severe hip pain and shoulder pain after hip and shoulder contusions 4 hours after a bicycle accident. No fractures or a head injury. Which opioid would you choose for treatment and why?
oral hydrocodone (opioid use for acute pain)
32-year-old woman with uncontrolled rheumatoid arthritis while on DMARD (disease modifying antirheumatic drug) and severe polyarthralgias, is still experiencing severe pain every 3 to 4 hours after taking moderately high does oxycodone on for more than two weeks. Which opioid would you choose to give this patient?
Oxycodone extended release oral (Chronic pain opioids) -last 3-4 hours but extended release mean release for 12 hours -taking more than 2 weeks mean tolerance build up
35-year-old woman with the right femoral fracture that occurred after a fall injury. He is on buprenorphine/naloxone sublingual and clinic record support good control of her opioid use disorder. You recognize the obvious need for opioid to manage her severe pain prior to admission to orthopedics for urgent surgical internal fixation. Which opioid would you choose?
-Fentanyl IV -Need to treat with something with higher affinity, because she is on buprenorphine which has such a high affinity.
23-year-old male methadone user had a witnessed overdose and was transported to your ED following a bystander administration of Evzio (naloxone hydrochloride injection). He is awake and in acute withdrawal, but while in the ED he becomes increasingly more sedated. Why?
Naloxone is short acting and methadone is long acting, so methadone OD symptoms return after naloxone metabolized -give naloxone IV and wait til methadone clears
46-year-old man with severe pain immediately after surgery for partial colon resection, following ruptured diverticulitis. Nausea and vomiting from post op. Has hypomotility of the gastrointestinal tract in the absence of mechanical bowel obstruction. Which opioid would you choose?
- morphine IV -no addiction problems -oral route won’t work because vomitting -(can’t give fentanyl transdermal because takes to long to clear, get stuck in fat)
How do volatile anesthetics work?
-Decrease effectiveness of excitatory transmission (glutamatergic) -increasing effectiveness inhibitory (GABArrgic) -effect throughout CNS
2 year old need ear tubes what anesthetic use?
-Sevoflurane (can breathe in when awake and make smell good) -Can’t use desflurane because volatile, so child won’t breathe in when awake
Minimal alveolar concentration (MAC)
ED 50, dose 50% effectiveness -Age best predictor (need lower dose) body -weight and gender doesn’t effect -measurement of anesthetic dose
What measurement of MAC cause perception amnesia, but patients are MAC aware
.25-.30 MAC
What MAC level make patients unconsc , MAC asleep?
.4-.5 MAC
What level MAC cause immobility?
1.0 MAC
Partial fraction for drugs effecting brain
1.4 times more in blood than lungs 2.2 amount of blood needed to effect brain
If targeting brain for drug what would decrease the onset of drug effect?
Increase fat solubility= decrease how quick reach brain
22 year old need dental work, what medication use?
NO, -Rapid onset, odorless, tasteless, low potency - don’t use if patient has pernicious anemia (inhibit enzymatic action of B12) SAE: nausea and vomiting
Ethers do what?
- Increased respiratory rate, decreased title volume. - all halogenated ethers cause vasodilation, decreased myocardial contractility, and generally decrease blood pressure
All halogenated ethers can trigger what bad side effect that is very important to know? Can happen hours after exposure?
Malignant hyperthermia: ca2+ channel problem 1. Elevated core body temperature with rigidity 2. Severe metabolic acidosis 3. Multi organ system failure
Treatment for malignant hyperthermia
Dantrolene
Drug that kills people through respiratory depression via induce cytochrome p450 system
Sodium thiopental
An infant is having trouble with seizures. What kind of drug can be used?
Phenobarbital (can also be used for alcohol withdrawal occasionally)
Name the barbiturates that are used in the US today.
Phenobarbital and butalbital (HA), if combine with alcohol or other sedative = respiratory depression and death -high risk of OD and respiratory distress
And eight-year-old child with severe epilepsy has developed a prolonged seizure that has been lasting for over 20 minutes. You see no good targets for an IV, how will you stop her seizure?
Ativan/lorazepam (benzodiazepines), nasal or rectal
What are the effects of benzodiazepines?
Sedation, hypnosis, anxiolytics, muscle relax station, amnesia. - this drug acts through the GABA receptor - can be given orally, IM, IV, or rectally
Long acting benzodiazepines
Diazepam (Valium): - highly lipid soluble, long half life (1-2 days) -tx: anxiety, muscle spasms, or in a reptile gel for status epilepticus
Ativan treatment for…
Anxiety, agitation, status epilepticus ( can interfere with memory formation)
22-year-old female, healthy, with CT demonstrated acute appendicitis. She is terrified of surgery. How are you going to premedicate for anesthesia?
-midazolam (versed) Short half life (1.5-2hrs)
What do you NOT want to give to a patient that is on a benzodiazepines?
Opioids, would cause severe respiratory depression which can be life threatening
Propofol
Brief sedation, wake up in 9 minutes -GABA receptor -drops bp fast, don’t use on hypotensive patients
82-year-old female, Tachycardic, hypotensive, in need of urgent debridement of infected left foot wound. What drug give for sedation?
Etomidate - won’t drop bp, minimal impact on heart -suppression of adrenal function -act via GABA
52 your old male, with the leg that needs irrigation, he Bridgman, and complex laceration repair. You don’t have any local anesthetic or anesthesia machine. You are in South Sudan. How will you induce anesthesia?
Ketamine: -Rapid onset and offset -acts NMDA receptor -“dissociative state” -no effect respiration, but increases salvation, HR, and bp -cause bad hallucinations
31-year-old female on third trimester of pregnancy is scheduled for an urgent right heart catheterzation. Patient has a history of pulmonary hypertension, and chronic hypoxemia. Sedation and general anesthesia pose risk for aspiration, placental transfer of drugs, hemodynamic and possible need of emergency C-section.
Can use a local anesthetic
Local anesthetic MOA
-target Voltage gated Na+ channels (block channels INSIDE cell) - prevents conduction an electrically tissue (nerves, myocardium, vascular smooth muscle) -block small myelinated nerves (pain and temperature) easily
Lidocain
Local anesthetic -rapid onset, medium duration -safe Water soluble
Bupivacaine
Local anesthetic -slower onset, long duration - potential serious cardiac toxicity Lipid soluble
Local anesthetic toxicity
*CNS-seizures, respiratory depression *Myocardium- arrhythmia, myocardial Vasodepression *Water soluble (CNS>>>cardiac toxicity) *lipid soluble (CNS toxicity = cardiac toxicity) ventricle arrhythmias
You need to perform surgery but the patient keeps moving. what can you give him to help immobilize the patient or to make him still for ventilation?
Neuromuscular blocker
Neuromuscular blockers
Only block nicotinic acetylcholine receptor at endplate of muscle (target only skeletal muscle)
You are planning on anesthetizing a 21 year old male for a short bronchoscopy procedure (20 minute). He will need an endotracheal tube. Do you choose a depolarizing or nondepolarizing neuromuscular blockers? What if the surgery was scheduled for two hours?
Depolarizing for short (b/c short onset) and non depolarizing for long surgery.
Succinylcholine
-Depolarizing neuromuscular blocker - Rapid onset, Ultra short acting -can cause malignant hyperthermia
Cerebellum damage
- Loss coordination, posture, and balance on same side of damage
- uses sensory input
- damage doesn’t cause sensory loss or muscle weakness
