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Pharmacology > Drugs Against Pain > Flashcards

Drugs Against Pain Flashcards

1
Q

Ether

A
  • Inhalation anesthetic, slow on set and recovery (obsolete)
  • Post operative nausea and vomiting
  • highly explosive
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2
Q

Nitrous oxide

A
  • Low potency, combined with other agents
  • good analgesic
  • Rapid induction and recovery
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3
Q

Halothane

A
  • Inhalation anesthetic
  • Potent non-explosive, non-irritant
  • 30% metabolized in liver, repeated use causes liver damage
  • No analgesic properties
  • Causes hypotension(vasodilator, cardio-supression)
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4
Q

Enflurane

A
  • Similar to halothane, inhalation anestetic
  • Less metabolized-> less chance of liver damage
  • Also: Isoflurane, Sevoflurane, Desflurane
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5
Q

Thiopental

A
  • IV anesthetic, Barbiturate
  • High lipid solubility
  • Rapid action, accumulates in fat
  • No analgesic effect, narrow therapeutic range
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6
Q

Propofol

A
  • IV anesthetic, rapid metabolism->quick recovery
  • Drug of choice for day surgery
  • Continuous infusion
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7
Q

Ketamine

A
  • IV anesthetic, Phencyclidine analogue
  • Good analgesia, and amnesia
  • Hallucinations during recovery
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8
Q

Midazolame

A

-IV anesthetic, Benzodiazepine

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9
Q

Modern Anesthesia Cycle

A
  • Premedication: Anxiolytic-> Diazepam(diazepines), Analgesic-> Pentazocine(opioid), Autonomic stabilization->Atropine (muscarinic antagonist prevents visceral reflexes)
  • Introduction: Unconsciousness/amnesia-> Midazolame (benzodiazepine), Muscle relaxation/intubation->Succinylcholine (nicotinic antagonist),
  • Maintenance: Inhalation anesthetic-> enflurane, anelgesic-> N2O, Muscle relaxant-> Pancuronium
  • Recovery: Reversal of neuromuscular block-> neostigmine, Pentazocine-> analgesia
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10
Q

Name and describe the three Opiate receptor subtypes

A
  • Serpentine Galpha i or ion channel
  • Mu-> most morphine effects
  • Delta-> reduce GI motility and respiratory suppression
  • Kappa-> mediate dysphoria and contribute to sedation, weak analgesic
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11
Q

Opiate spinal analgesia mechanism

A

-Activation of presynaptic opioid receptors-> decrease in presynaptic Ca-> decreased neurotransmitter release-> decreased transmission of nociception

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12
Q

Opiate supra spinal analgesia

A

-Activation of post synaptic opioid receptors in medulla and midbrain-> increase K+ flux-> inhibition of neurons in pain pathway

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13
Q

Name 2 endogenous opioids

A

-Endorphins, enkephalin

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14
Q

Effects of morphine

A
  • Sedation and drowsiness
  • Nausea
  • Cough suppressant(antitussive)
  • Pupillary constriction
  • Respiratory suppression, and depression of hypoxic drive
  • Increased GI tone-> segmentation, Decreased peristalsis-> constipation
  • Increased smooth muscle tone-> urinary retention
  • Withdrawal: autonomic hyperactivity-> diarrhea, vomiting, cramps pain
  • Caused by up regulation of AC due to reduced cAMP during use
  • Eliminated by glucuronidation
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15
Q

Codeine

A
  • Opioid, Converted to Morphine by demethylation via CYP2D6 (inhibited by fluoxetine, 10% of pop. mutated-> resistance)
  • Better oral absorption than Morphine
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16
Q

Dextromethorphan

A
  • Synthetic morphine derivative
  • Equally antitussive
  • No analgesia or GI effects, doesn’t act through opioid receptors
17
Q

Heroin

A
  • Diacetylated morphine
  • 2x more potent than morphine
  • Higher lipophilicity-> crosses blood brain barrier quickly-> greater rush
18
Q

Hydrocodone

A
  • Opioid

- Vicodin, often combined with NSAID’s

19
Q

Oxycodone

A

-Opioid, slow release formula for chronic pain

20
Q

Meperidine

A
  • Opioid analgesic

- Shorter duration used during labour

21
Q

Methadone

A
  • Opioid

- Long duration >24hrs-> less psychological dependance

22
Q

Etorphine

A
  • 1000x morphine

- Large animal tranquilizer

23
Q

Fentanyl

A
  • Opioid, high potency (transdermal)

- Short lasting: anesthesia, patient controled infusion

24
Q

Nalaxone

A
  • Opiate antagonist
  • Short acting
  • Treat overdoses and improve breathing in new borns
  • Induce severe withdrawal symptoms
25
Q

Naltrexone

A
  • Opiate antagonist
  • Longer duration
  • Prevent addict relaps
26
Q

Local Anesthetic Mechanism

A
  • Reversibly block Na channels intracellularly(can’t be ionized), only active when ionized
  • Weak base ionized at physiological pH
  • High affinity for open/inactive channels (inflamed damaged tissue higher pH-> too ionized, can’t get inside cell)
  • High effect-> sensory, Med effect-> Sympathetic nerves, Low effect-> somatic nerves
27
Q

Ester Local Anesthetics

A
  • Cocaine, Procaine, Benzocaine, Tetracaine
  • Benzene ring attached to basic side chain
  • Shorter lasting, inactivated by nonspecific esterases
28
Q

Amine Local Anesthetics

A
  • Lidocaine, Prilocaine, Bupivacaine
  • Longer lasting
  • Administered with vasoconstrictors-> maintain at injection site
29
Q

Nonselective NSAID’s

A

-Asprin (acetyl-salicylic acid), Acetaminophen, Ibuprophen, Naproxen, Diclofenac, Indomethacine

30
Q

Cox-2 selective NSAID’s

A
  • Increased risk of heart disease

- Rofecoxib, Celecoxib, Valdecoxib

31
Q

NSAID mechanism and effect

A
  • Cyclo-oxygenase inhibitors
  • IL-1 from macrophages induces COX-2 in brain-> PG E produced-> effects thermo regulation-> fever, PG’s also sensitize pain receptors
  • Increase in Leukotrienes-> Bronchial constriction
  • Decrease prostacyclin (PG)-> less mucosal dilation-> more acid-> ulcers
  • COX-1 inhibition-> side effects-> gastrointestinal, bronchial spasm

Pharmacology (10 decks)

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