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CCOM Pharm Exam 3
Pharm
61
Pharmacology
Professional
10/11/2010

Additional Pharmacology Flashcards

 


 

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Term
Morphine
(Action)
Definition
mu agonist
Term
Codeine
Definition
mu agonist

USE: -Mild pain relief

KINET: -Much less 1st pass metabolism than morphine
Term
Fentanyl
Definition
mu agonist

KINET: -100X potency of Morphine
Term
Heroin
Definition
mu agonist

USE: Abuse

NOTES: -Schedule 1 Drug (no medical use allowed)
Term
hydrocodone
Definition
mu agonist

USE: -most widely used opioid

NOTES: -component of Vicadin (also contains Acetominophen) and loritab
Term
hydromorphone
Definition
mu agonist

USE: -similar to morphine
Term
Meperidine
Definition
mu agonist

NOTES: -Rarely used
Term
Methadone
Definition
mu agonist

USE: -Tx of heroin withdrawal, chronic severe pain
Term
Oxycodone
Definition
mu agonist

USE: -chronic Tx of severe pain

NOTES: -"percocet" OxyContin (slow release, widely abused; "hillbilly heroin")
Term
Propoxyphene
Definition
mu agonist

NOTES: -low abuse potential, not much better than placebo
Term
Pentazocine
Definition
mu partial agonist (agonist/antagonist) -- Stronger KAPPA agonist ;. decreased pain

USE: Tx of moderate pain

NOTES: Stimulates kappa receptor. Less abuse potential because it stimulates mu recptors less
Term
Buprenorphine
Definition
partial mu agonist (agonist/antagonist)

USE: Tx of moderate pain & Tx of opioid addiction

NOTES: -highly used right now. Enough Mu agonist activity to prevent withdrawal effects
Term
Butorphanol
Definition
mu partial agonist (agonist/antagonist)

USE: -moderate pain
Term
Tramadol
Definition
mu partial agonist (agonist/antagonist)

USE: -moderate pain

MECH: -partial mu agonsist, NT-RI activity (similar to antidepressant activity)

NOTES: -Newer drug
Term
Naloxone
Definition
mu antagonist

USE: Tx of opioid poisoning

MECH: Mu antagonist (No agonist activity)

KINET: Fast acting (IV admin)
Term
Naltrexone
Definition
mu antagonist

USE: Tx of addiction (poor results)

KINET: Longer acting oral admin
Term
Methylnaltrexone
Definition
mu antagonist

USE: Prevents opioid-induced constipation

MECH: Quaternary opioid antagonist (;. no CNS activity)

NOTE: New drug
Term
Phenytoin
Definition
Antiepiletic Drug (old standard)

Mech: Inhibits voltage gated Na channels

Use: Monotherapy for Tonic/clonic Sz & Partial Sz

Kinetics: 90% plasma protein bound
-dose increases disproportionately increase the available amount of drug
-must monitor levels to ensure proper blood doses
-95% liver metabolism (CYP2C9, -2C10, -2C19)

SE: Gingival hyperplasia (20% PTs on long term therapy)
-Steven Johnson Syndrome (blistering of skin & mucous membranes) - not restricted to anticonvulsants
-severe for of SJS called Toxic epidermal necrosis
--Cease Tx if occurs!
Term
Carbamazepine
Definition
Antiepiletic Drug (old)
-inhibits voltage gated Na channels
-also Tx of Neuropathic pain

Kinetics: -metabolism difficult to predict (like Phenytoin

SE: -Stupor coma hyperirritability & Increased
Term
Ethosuximide
Definition
Antiepiletic Drug (old)
-Inhibits 'T-type calcium channels' (Absence Sz ONLY)
-Few drug drug interactions
Term
Valproic Acid
Definition
Antiepiletic Drug (old)

USE: -Treats ALL types of Sz (including Absence)
-inhibits voltage gated Na channels, also...
-Inhibits 'T-type calcium channels'

SE: -Causes heptotoxicity
Term
Benzodiazepines
Definition
Antiepiletic Drug (old)
-Enhance GABA-A's inhibitory effects (post-synaptic)
-controls status epilepticus
--Used as ADJUNCTIVE Tx (Not monotherapy)
Term
Clonazepam
Definition
Antiepiletic Drug (Benzodiazepine - old)
Term
Clorazepate
Definition
Antiepiletic Drug (Benzodiazepine - old)
Term
Gabapentin
Definition
Antiepiletic Drug (New)

USE: -Tx of Partial Sz
-used in Tx of Neuropathic Pain
--Adjunctive Tx

MECH: -Mimics gaba shape, not action

KINET: Excreted unchanged in urine (:. Check urine function)

Factoid: - Whistleblower for off-label promotion
Term
Oxcarbazepine
Definition
Antiepiletic Drug (New)
-inhibits voltage-gated Na channels
Term
Lamotrigine
Definition
Antiepiletic Drug (New)

USE: -Mono or Adjunctive Tx for partial and general Tonic/Clonic
-Tx of LGS

MECH: -Slow recovery of voltage-gated Na channels (ie phenytoin)
-Inhibit some Ca channels

KINET: Alters other drugs' T1/2
- Long T1/2 (~24 hours)

SE: SJS (adjunctive Tx), Dizziness, Ataxia
Term
Levatiracetam
Definition
Antiepiletic Drug (New)
-Also Tx of Bipolar Disorder
Term
Ergotamine Tartrate
Definition
Ergot alkyloid/Act on 5-HT receptor

USE: -
MECH: -

KINET: Taken orally, sublingually, or by suppository

SE: -
Term
Dihydroergotamine
Definition
Ergot alkyloid/Act on 5-HT receptor
USE: -
MECH: -
KINET: -
SE: -
Term
Methysergide Maleate
Definition
Ergot alkyloid/Act on 5-HT receptor
USE: -
MECH: -
KINET: -
SE: -
Term
Sumatriptan
Definition
5-HT (1B/1D) Agonist USE: - MECH: - KINET: - SE: -
Term
Zolmitriptan
Definition
5-HT (1B/1D) Agonist
USE: -
MECH: -
KINET: -
SE: -
Term
"-triptan" refers to which drugs?
Definition
5-HT (1B/1D) Agonist
Term
Metoclopramide
Definition
Dopmine ANTagonist (Antiemetic)
USE: -
MECH: -
KINET: -
SE: -
Term
Prochloperazine
Definition
Dopmine ANTagonist (Antiemetic)
USE: -
MECH: -
KINET: -
SE: -
Term
Midrin
Definition
Analgesic (acetominophen + steroid + synpathomimetic)

USE: Tx of migraines (1st line)

MECH: - multiple, includes vasoconstriction

KINET: - 1/hr, up to 6/day

SE: - Very few
Term
"-olol" beta blockers
Definition
USE: -
MECH: -
KINET: -
SE: -
Term
Amitriptyline
Definition
Antidepressant
USE: -
MECH: -
KINET: -
SE: -
Term
Valproate
Definition
Antiseizure Drug
USE: -
MECH: -
KINET: -
SE: -
Term
Topiramate
Definition
Antiseizure Drug
USE: - Migraine prophylaxis
MECH: -
KINET: -
SE: -
Term
Gabapentin
Definition
Antiseizure Drug
USE: -
MECH: -
KINET: -
SE: -
Term
What effect does mu receptor signaling produce?
Definition
Strong analgesia
Abuse potential
respiratory depression
Term
Mu Opioid Receptor
(Location & Effects)
Definition
Brainstem, spinal, and limbic

EFFECTS: Limbic Effects, some spinal effects, Supraspinal effects, sedation, resp. depression, dependence
Term
Kappa Opioid Receptor
(Location & Effects)
Definition
Brainstem & Spinal

EFFECTS: Some spinal, some supraspinal, sedation, & Dysphoria
Term
Delta Opioid Receptor
Definition
Term
Endorphins & Enkephalins
-How do they trigger receptors?
Definition
Structurally similar to Opioids
Term
Fosphenytoin
Definition
Term
NSAIDs
Definition
Use: Suppress acute attack of gout
Term
Colchicine
Definition
USE: Suppress acute attack of gout
Term
Prednisone
Definition
USE: Suppress acute attack of gout
Term
Methylprednisone
Definition
USE: Suppress acute attack of gout
Term
Probenecid
Definition
USE: Increase excretion of Uric Acid
Term
Allopurinol
Definition
USE: Inhibit the formation of uric acid
Term
Febuxostat
Definition
USE: Inhibit the formation of Uric Acid
Term
Morphine
(Use)
Definition
USE: -Analgesia (acute - trauma & chronic - cancer)

-Sedation & mental clouding (not classic sedative effects)
---Easily aroused from "floating dream-like" sleep
---OD can lead to stupor, coma or death

-Antitussive Effects (ie codeine) however they can degranulate mast cells which is VERY BAD for asthmatics

-Adjunct to surgical anesthesia

-Antidiarrheal derivatives (Loparamide - immodium)

-Abuse

NOTE: Administered as infusion, PCA (gold standard for pain management), or spinal anesthesia admin
Term
Morphine
(Kinetics)
Definition
KINET: ~75% 1st pass metabolism if oral therefore usually parenteral administration (usually sustained release)

-*Standard dose: 10 mg subQ or IM* (lower amount when IV)

-Rapid onset of action, short duration (4-6hrs)

-Glucuronide metabolism

-Cross BBB & placental barrier (abuse affects fetus)
Term
Morphine
(Side Effects)
Definition
SE: -Euphoria (typically) via reward centers. Rarely dysphoria, affecting mainly females
-Nausea via CRTZ activation (sometimes treatable), which reduces w/ tolerence
---vestibular component of nausea may exist
-Respiratory depression (rate & depth) at therapeutic dose (may exacerbate resp. problems)
-Decreases sensitivity of chemo CO2 receptors (reduced drive to breath) ;. respiration is based solely on hypoxic response---;. can stop breathing if O2 is administered
-Constriction of pupils ("pin point pupils") - not affected by tolerance
-Antitussive Effects
-Histamine release causes itch over the skin (;. antihistamines (diphenhydramine) used to alleviate itch)
-Increased risk of seizures
-Chronic high dose - endocrine, and other effects
-Deceased bowel motility (constrict circular, relaxed longitudinal) = constipation;. laxatives (osmotic laxatives like miralax or milk of magnesia) may help
-urine retention (another smooth muscle effect) - may need to catheter for drainage
-Bronchoconstriction (via histamine effect, not mu receptor)
-Constriction of sphincter of oddi (decreased bile bladder contraction) - helps with pain, exacerbates cholistitis
-Cardiovascular effects (postural hypotension - histamine mediated)
-Cutaneous vasodilation (flushing) - Cold turkey skin with withdrawal
-increase ICP (hi CO2 --> vasodilation) ;. don't use with closed head injuries if avoidable
-Immunosuppression w/ chronic use (assumed to be effect of heroin early in Hx of AIDS)
Term
Morphine
(Miscelaneous Notes)
Definition
NOTES: -A Classic drug
-Rage attacks in cats
-Re Pulmonary Edema w/ MI: decreases anxiety which is exacerbating cardiopulm. problems
---also some vasodilation effects
Term
Morphine
(Interactions)
Definition
Interactions:
-CNS depressants have additive effects
-cocaine/heroin + morphine = speedball (Belushi)
-Useful when given with painkillers of different types (ie - mu & COX effects)
-Increased analgesia when given with antihistamines
-Tricyclic antidepressants also enhance effects of opioids
Term
Morphine
(overdose)
Definition
Overdose: Opioid Antagonist - can't hurt the patient if wrongly diagnosed. ALso give respiratory support
Toxidrome: Stupor, bradypnea, Pin-point pupils
---fixed and dilated pupils indicate hypoxia and imminent death
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