Pharm - Second Packet
Terms
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- Nicotine
- - binds peripheral and central nAchRs with biphasic effects
- Bupropion
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- 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
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- produces tolerance to heroin
- use with caution for pain relief, may cause respiratory failure in sensitized patient - LAAM
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- 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
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- oral THC
- used as an antiemetic, appetite stimulant, muscle relaxant, glaucoma, etc - MDMA
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- binds 5HT2A receptor
- combination of mescaline and methamphetamine - LSD
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- binds 5HT2A receptor
- no withdrawal symptoms or dependence
- tolerance develops quickly - PCP
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- noncompetitive NMDA antagonist and blocker of the associated Ca-channel
- treat toxicity with benzos or diazepam - Ketamine
-
- potent amnestic and analgesic
- causes sialorrhea, myocardial depression, sympathetic activation, hallucinations, and increased intracranial pressure - Lidocaine
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- 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
-
- prevents gastric ulceration
- approved for midtrimester abortions - Apirin (acetylsalicylic acid)
-
- irreversible COX inhibitor
- inhibits NF-kB, disrupts adhesion
- causes GI blood loss
- rarely causes Reye's syndrome in children - Acetominophen (Tylenol)
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- 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
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- 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
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- given for inflammatory bowel
- does not get absorbed systemically - N-acetylcystein
-
- antidote for acetaminophen toxicity
- repletes glutathione - Naproxen
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- used for dismenorrhea
- approved for RA, osteoarthritis, analgesia, fever - Salsalate
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- reversible inhibitor of COX, but weaker than ASA
- less GI and platelet effects than ASA - Sodium Salicylate
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- similar to salsalate (weaker than ASA, but less GI and platelet effects)
- also blocks NF-kB - Sulindac
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- 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
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- same effects as isoflurane
- lowest blood:gas partition coefficient (rapid sleep/wake)
- pungent, only used in maintenence - Sevoflurane
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- 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 - Etomidate
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- rapid sleep/wake
- very cardio-stable
- no effect on intracranial pressure
- used for head injuries - Side-effects of injection anesthetics
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- nausea/vomiting
- increased glucocorticoids/mineralicorticoids
- possibly myoclonis on injection