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56 Cards in this Set

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  • Back
Nicotine
- binds peripheral and central nAchRs with biphasic effects
Bupropion
- antidepressant, blocks NE & 5HT reuptake
- treats nicotine dependence
Cocaine
- local anesthetic, blocks Na-channels
- blocks reuptake of NE & DA peripherally
- blocks DA uptake in the nucleus accumbens
- no pharmacological treatment for addiciton
Amphetamines
- blocks DA reuptake and stimulates DA release
- enhances NE & 5HT
- longer lasting than cocaine
Heroin
- lipophilic form of morphine
- treat overdose with benzos, clonidine and others
Methadone
- produces tolerance to heroin
- use with caution for pain relief, may cause respiratory failure in sensitized patient
LAAM
- opioid agonist
- used to treat addiction
Buprenorphine
- partial agonist at mu, antagonist at kappa
- does not cause respiratory depression like morphine
- can produce euphoria when given IV
Naltrexone
- competitive mu and kappa antagonist
Ethanol
- general CNS depressant
- withdrawal may lead to grand mal seizures
- to detox: crossover to benzos then taper off
Disulfiram
- irreversibly inactivates aldehyde dehydrogenase
- leads to build-up of acetaldehyde = negative symptoms
- Antibuse
Barbituates & Benzodiazepines
- withdrawal from barbiturates is more severe than benzos or EtOH, there is cross-tolerance b/w the three
- barbiturates have a low therapeutic index, but can be used to manage benzo withdrawal
THC
- has a natural receptor in the brain
- increases DA in the nucleus accumbens
Marinol
- oral THC
- used as an antiemetic, appetite stimulant, muscle relaxant, glaucoma, etc
MDMA
- binds 5HT2A receptor
- combination of mescaline and methamphetamine
LSD
- binds 5HT2A receptor
- no withdrawal symptoms or dependence
- tolerance develops quickly
PCP
- noncompetitive NMDA antagonist and blocker of the associated Ca-channel
- treat toxicity with benzos or diazepam
Ketamine
- anesthetic
Lidocaine
- anesthetizes mucous membranes
- liver extracts 70% from the blood
Procaine
- hydrolyzed in plasma by pseudocholinesterase
- rarely used because of lidocaine
- novocaine
Bupivacaine
- may cause hypotention and collapse of the heart
- sometimes used in an epidural with fentanyl
Mepivacaine
- related to lidocaine
- sometimes used in epidural
Increasing concentration of local anesthetics will cause block of (in order):
1. somatic sensory/visceral motor
2. somatic motor/visceral sensory
3. motor nerves
PGI2 (prostacyclin)
- made in vascular tissues by prostacyclin synthase
- spontaneously degrades, not broken down in the lungs!
- uses cAMP
- vasodilation
- GI protection
- increase GFR
- hyperalgesia
- platelet aggregation
PGE2
- formed in most tissues w/o enzymatic help
- uses cAMP
- metabolized by PGDH in lungs
- some vasodilation
- GI protecting
- smooth muscle contraction (crams)
- increases GFR
- bronchodilates
- hyperalgesia
- midterm abortion
PGF2-alpha
- formed in most tissues (+/- enzymes)
- uses PLC
- metabolized by PGDH
- required for labor
- bronchoconstricts
TXA2
- made in platelets & lungs by thromboxane synthase
- uses PLC
- causes platelet aggregation
- causes brochoconstriction
LTB4
- made by PMNs
- uses PLC and cAMP
- causes edema
- platelet aggregation
- hyperalgesia
LTC4 & LTD4
- use PLC
- causes edema
- smooth muscle contraction
- LTC4 bronchoconstricts
Zileuton
- 5-lipoxegenase inhibitor
- treats rhinitis and asthma
Misoprostol
- PGE1 analogue
- supresses gastric ulceration
- used for midterm abortion
Apirin (acetylsalicylic acid)
- irreversible COX inhibitor
- inhibits NF-kB, disrupts adhesion
- causes GI blood loss
- rarely causes Reye's syndrome in children
Acetominophen (Tylenol)
- weak COX inhibitor, has other effects
- used when aspirin is contraindicated
Celecoxib
- selective COX-2 inhibitor
- similar analgesic and antipyretic effects as nonselectives, less GI complications
- block PGI2, but not TXA2, dysregulation of platelet homeostasis
Rofecoxib
- selective COX-2 inhibitor
- similar analgesic and antipyretic effects as nonselectives, less GI complications
- block PGI2, but not TXA2, dysregulation of platelet homeostasis
Diflunisal
- competitive inhibitor of COX
- used as analgesic
Ibuprofen
- non-selective COX inhibitor
- used for RA, osteoarthritis, analgesic, fever, patent ductus arteriosus
Indomethacin
- non-selective COX inhibitor
- used for patent ductus arteriosus
Ketorolac
- non-selective COX inhibitor
- given IM or IV post-surgically
- very similar to morphine or meperidine, but without tolerance
Mesalamine
- given for inflammatory bowel
- does not get absorbed systemically
Sulfasalazine
- given for inflammatory bowel
- does not get absorbed systemically
Misoprostol
- prevents gastric ulceration
- approved for midtrimester abortions
N-acetylcystein
- antidote for acetaminophen toxicity
- repletes glutathione
Naproxen
- used for dismenorrhea
- approved for RA, osteoarthritis, analgesia, fever
Salsalate
- reversible inhibitor of COX, but weaker than ASA
- less GI and platelet effects than ASA
Sodium Salicylate
- similar to salsalate (weaker than ASA, but less GI and platelet effects)
- also blocks NF-kB
Sulindac
- blocks COX and PPAR-delta
- beneficial for colon cancer
- long duration of action b/c of enterohepatic cycling
- approved for RA, osteoarthritis, ankylosing spondylitis
Nitrous Oxide
- alveolar ventilation is maintained
- mild myocardial depression
- activates sympathetic nervous system
- may impair DNA synthesis or increase the size of a pneumothorax
Halothane
- potent bronchodilator
- commonly used in pediatrics
- little effect on SVR
- increased: RR, EDP, intracranial pressure
- decreased: TV, baroreceptor function, sympathetic outflow, SA node automaticity
Isoflurane
- bronchodilator
- very irritating to airways, not used as an induction agent
- (+) chronotope, (-) inotrope
- decreased: SVR, BP
Desflurane
- same effects as isoflurane
- lowest blood:gas partition coefficient (rapid sleep/wake)
- pungent, only used in maintenence
Sevoflurane
- smooth, excellent for induciton
- cardio-stable
- low blood:gas coefficient (rapid sleep/wake)
- hydrolysis by soda lime may lead to toxic intermediates
Propofol
- rapid sleep/wake
- anti-emetic
- used for short procedures
Ketamine
- potent amnestic and analgesic
- causes sialorrhea, myocardial depression, sympathetic activation, hallucinations, and increased intracranial pressure
Etomidate
- rapid sleep/wake
- very cardio-stable
- no effect on intracranial pressure
- used for head injuries
Side-effects of injection anesthetics
- nausea/vomiting
- increased glucocorticoids/mineralicorticoids
- possibly myoclonis on injection