Katzung Chapter 30: Antidepressant Agents, Chapter 31: Opioid Agonists and Antagonists and Chapter 32: Drugs of Abuse

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62 Terms

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Mu opioid receptor

Stimulation produces analgesia, euphoria, respiratory depression and physical dependence

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Delta opioid receptor

Stimulation produces analgesia

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Kappa opioid receptor

Stimulation produces analgesia

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Tolerance

With frequently repeated administration of therapeutic doses of opioids there is a gradual loss in effectiveness

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Physical Dependence

Occurrence of a withdrawal or abstinence syndrome when the drug is stopped or an antagonist is administered

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Hyperalgesia

Persistent administration of opioid analgesics has been observed to increase the sensation of pain

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Morphine

Strong naturall occuring opioid agonist from the poppy plant (Papaver somniferum), binds with high affinity to the mu opioid receptor

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Buprenorphine

High binding affinity but low intrinsic activity at the mu opioid receptor, antagonist at the delta and kappa receptors, combined with nalaxone for the treatement of opiate addiction

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Neuraxial

Injection of an anesthetic drug into the fatty tissue that surround the nerve roots (epidural) or into the cerebrospinal fluid (spinal)

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Fentanyl

Strong opioid agonist, available as a sustained release, transdermal patch (3 days), indicated for the management of persistent unremitting pain, because of respiratory depression, FDA recommends a fentanyl patch (25 mcg/h) be reserved for patients with an established oral morphine requirement of at least 60 mg/d for 1 week or more

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Butorphanol

Kappa receptor agonist, may be a mu receptor partial agonist or antagonist, available as intranasal preparation

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Nalaxone

Opioid antagonist, used to treat opioid overdose, has a short half-life so it needs to be administered frequently

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Hydromorphone

Strong opioid agonist

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Heroin

Strong opioid agonist

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Methadone

Strong opioid agonist, has a longer half-life, used for detoxification

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Levorphanol

Strong opioid agonist

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Codeine

Mild to moderate opioid, partial agonist that is usually combined with aspirin or acetaminophen

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Oxycodone

Mild to moderate opioid, partial agonist that is usually combined with aspirin or acetaminophen

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Hydrocodone

Mild to moderate opioid, partial agonist that is usually combined with aspirin or acetaminophen

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Loperamide

Mild opioid agonist, used for diarrhea

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Tramadol

Centrally acting analgesic, blocks serotonin reuptake and is a weak mu receptor agonist

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Dextromethorphan

Oioid agonist with antitussive actions but little or no CNS effects, not for use in children under 6 years old

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Naltrexone

Opioid natagonist with a longer duration of action used in alcohol and nicotine abstinence programs

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Ziconotide

Blocks N type, voltage gated calcium channels and prevents release of neurotransmitters, apprved for chronic pain (intrathecally)

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Methylnaltrexone

Opioid antagonist, used to treat opioid-induced constipation

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Alvimopan

Opioid antagonist, used to treat postoperative ileus

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Tricyclic antidepressant

Block the reuptake of norepinephrine and/or 5-HT into the presynaptic membrane

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Amitriptyline

Tricyclic antidepressant

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Imipramine

Tricyclic antidepressant

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Selective Serotonin Reuptake Inhibitors

Greater ability to block the reuptake of serotonin (5-HT) compared to norepinephrine reuptake

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Fluoxetine

Antidepressant, Selective Serotonin Reuptake Inhibitors

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Paroxetine

Antidepressant, Selective Serotonin Reuptake Inhibitors

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Sertraline

Antidepressant, Selective Serotonin Reuptake Inhibitors

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Citalopram

Antidepressant, Selective Serotonin Reuptake Inhibitors

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Escitalopram

Antidepressant, Selective Serotonin Reuptake Inhibitors

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Fluvoxamine

Antidepressant, Selective Serotonin Reuptake Inhibitors

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Venlafaxine

Antidepressant, blocks reuptake of both norepinephrine and serotonin

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Desvenlafaxine

Antidepressant, blocks reuptake of both norepinephrine and serotonin

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Duloxetine

Antidepressant, blocks reuptake of both norepinephrine and serotonin

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Levomilnacipran

Antidepressant, blocks reuptake of both norepinephrine and serotonin

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Milnacipran

Antidepressant, blocks reuptake of both norepinephrine and serotonin

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Bupropion

Antidepressant and used in smoking cessation, modest-to-moderate inhibitor of norepinephrine and dopamine reuptake, more significant effect is presynaptic release of catecholamines

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Trazodone

Antidepressant, 5HT2 receptor antagonist

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Mirtazapine

Antidepressant, mechanism is unknown

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Lithium

Used to treat manic/depressive disorder (bipolar), inhibition the inositol triphosphate (IP3) second messenger system

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Addiction

Compulsive drug-seeking behavior and cravings and for a drug for personal satisfaction

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2-arachidonyl glycerol

Endogenous cannabinoids, bind to presynaptic CB1 receptors and inhibit the release of glutamate and GABA

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Anandamide

Endogenous cannabinoids, bind to presynaptic CB1 receptors and inhibit the release of glutamate and GABA

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Dronabinol

Prescription Delta 9-tetrahydrocannabinol

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f-Hydroxybutyric acid

Bind to GABA-b receptors (metabotropic) activating potassium channels and causing hyperpolarization

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Nicotine

Influx of sodium ions after stimulation of acetylcholine ion channels

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Cocaine

Blocks reuptake transporters (dopamine, NE and 5HT) in the CNS

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Methylenedioxymethamphetamine

Release of biogenic amines by reversing the actions of transporters similar to amphetamines but with a preference for the serotonin transporter (SERT)

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Lysergic diethylamide

5HT2a receptor agonist in the prefrontal cortex enhancing glutamate transmission

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Mescaline

From peyote, 5HT2a receptor agonist in the prefrontal cortex enhancing glutamate transmission

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Psilocybin and psilocin

From mushrooms, 5HT2a receptor agonist in the prefrontal cortex enhancing glutamate transmission

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Phencyclidine

Use dependent inhibition of glutamate receptors, produces dissociative anesthesia

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Ketamine

Use dependent inhibition of glutamate receptors, produces dissociative anesthesia

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Nitrous oxide

Nitrates that is used as an inhalant, dilates blood vessels

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Amyl nitrate

Nitrates that is used as an inhalant, dilates blood vessels

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Benzene

Aromatic hydrocarbon used as an inhalant

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Toluene

Aromatic hydrocarbon used as an inhalant