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CNS Pharmacology
PHAR450
52
Pharmacology
Undergraduate 4
04/01/2014

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Term
Diazepam
Definition
Benzodiazepine (aka Valium)
Sedative-hypnotic
Also used to treat epilepsy, esp. status epilepticus
Term
Buspirone
Definition
5-HT1A receptor agonist
Anxiolytic with little or no sedation
Term
Thiopental
Definition
Barbiturate
No longer used as a sedative-hypnotic
Used as an anesthetic (i.v.)
Term
Phenobarbital
Definition
Barbiturate
No longer used as a sedative-hypnotic
Used as an anticonvulant
Term
Propanolol
Definition
Beta-adrenergic antagonist
Used to treat forms of anxiety with physical symptoms (e.g. sweating)
No effect in the affective component
Term
Chloral hydrate
Methaqualone
Definition
Sedative-hypnotic drugs
Miscellaneous
Term
Clonazepam
Definition
Benzodiazepine
Sedative-hypnotic
Also used to treat epilepsy
Term
Flurazepam
Definition
Benzodiazepine
Sedative-hypnotic
Also used to treat insomnia but replaced by Lorazepam
Long half-life, potential for "drug hangover"
Term
Lorazepam
Definition
Benzodiazepine
Sedative-hypnotic
Also used to treat insomnia, shorter half-life than flurazepam
Term
Flumazenil
Definition
Benzodiazepine antagonist
Reverses the effects of BZ acute overdose
Term
Ethanol
Definition
General CNS depressant
Acute use: affects primarily the CNS (e.g. disinhibition, motor ataxia, slurred speech)
Chronic use: affects other organ systems & adversely affects the fetus (e.g. FASD)
Term
Amphetamine (Dexedrine)
Methamphetamine (Methedrine, Speed)
Definition
Psychomotor stimulant
Competitively inhibits DAT & VMAT, increases extracellular DA
Term
Methylphenidate (Ritalin)
Definition
Psychomotor stimulant
Competitively inhibits DAT & VMAT, increases extracellular DA
Clinical use in ADHD
Term
Cocaine
Definition
Psychomotor stimulant
Inhibits DAT, increases extracellular DA
Used as a topical (local) anesthetic & recreationally
Rapid distribution and elimination, thus short duration of action
Term
Caffeine
Definition
Methylxanthine
Psychomotor stimulant most widely used
Blockade of adenosine receptors, inhibits PDE thereby increasing cAMP
Term
Theophylline
Definition
Methylxanthine
Psychomotor stimulant
Blockade of adenosine receptors, inhibits PDE thereby increasing cAMP
Term
LSD
Definition
Psychotomimetic drug
Produces schizophrenia-like symptoms
Term
Ectasy
Definition
Psychotomimetic drug
Term
Cannabis
Definition
Psychotomimetic drug
Actions produced by THC, including withdrawal symptoms
Term
Reserpine
Definition
Alkaloid
Depletes brain monoamines & precipitates depressive symptoms
Term
Impiramine
Amitriptyline
Definition
Tricyclic antidepressant(1st gen)
Inhibition of NE & 5-HT reuptake
As effective as SSRIs but more side effects
Term
Bupropione
Trazodone
Definition
2nd/3rd gen antidepressants
Mechanism of action unknown
Weak inhibitors of monoamine reuptake
Term
Fluoxetine
Definition
Selective serotonin reuptake inhibitor
Increases 5-HT in the synaptic cleft
May promote desensitization of 5-HT autoreceptor (negative feedback)
As effective as TCAs but less side effects
Term
Tranylcypromine
Phenylzine
Definition
Monoamine oxidase inhibitor
Original antidepressant
Inhibition of both MAO-A (metabolizes NE and 5-HT) & MAO-B (metabolizes DA) in CNS & periphery
Increases monoamine availability
Secondary downregulation of post-synaptic monoamine receptors
Used to treat severe depression
Term
Lithium ion (Lithium carbonate)
Definition
Mood stabilizer (classical drug)
Decreased NE release, increased NE reputake
Stabilization of alpha adrenoreceptor sensitivity to NE via interference with phosphatidylinositol pathway
May be added to antidepressant (bipolar illness) or antipsychotic (schizoaffective disorders) therapy
Low therapeutic index
Term
Valproic Acid
Definition
Mood stabilizer (newer drug)
Used to treat mania and biopolar illness
Also used as an anticonvulsant
Term
Phenycyclidine
Ketamine
Definition
NMDA receptor antagonist
Precipitates negative symptoms of schizophrenia
Term
Chlorpromazine
Definition
Typical antipsychotic drug
D2>D1
More adverse effects than atypical group
Term
Haloperidol
Definition
Typical antipsychotic drug
D2>>D1
More adverse effects than atypical group
Term
Clozapine
Definition
Atypical antipsychotic drug
5-HT2>D1=D2
Less adverse effects than typical group
Higher efficacy in treatment-resistant patients and negative symptoms
Term
Risperidone
Definition
Atypical antipsychotic drug
5-HT2>D2
Less adverse effects than typical group
Higher efficacy in treatment-resistant patients and negative symptoms
Term
L-DOPA
Definition
Precursor of DA
Most effective agent in treating PD
Often used with DOPA decarboxylase inhibitor or else distribution would be <1%
Term
Carbidopa
Definition
DOPA decarboxylase inhibitor
Often used with DA to treat PD
Term
Bromocriptine
Definition
DA Dreceptor agonist
Used in the treatment of PD
Term
Tolcapone
Entapapone
Definition
COMT inhibitor
Used in the treatment of PD
Inhibits DA metabolism
Term
Selegiline
Definition
Irreversible MAO-B inhibitor
Used in the treatment of PD
Inhibits DA metabolism
Term
Amantadine
Definition
Antiviral agent
Used for prophylaxis & treatment of influenza A, & PD
Releases DA from nerve terminals
Term
Benzotropine
Definition
Muscarinic AchR antagonist
Used in the treatment of PD (esp. resting tremor) before the development of L-DOPA when PD was thought to be caused by an imbalance of DA and Ach
Term
Morphine
Definition
Natural opioid agonist
Long-acting
Used to treat dyspnea from pulmonary edema associated with left ventricular failure
Term
Codeine
Definition
Natural opioid agonist
Long-acting
Term
Heroin
Definition
Semi-synthetic opioid agonist
Probably long-acting
Term
Hydromorphone
Definition
Semi-synthetic opioid agonist
Long-acting, most potent
Term
Oxycodone
Definition
Semi-synthetic opioid agonist
Long-acting
Term
Meperidine
Methadone
Definition
Synthetic opioid receptor agonist
Long-acting
Term
Fentanyl/Afentanyl
Definition
Synthetic opioid receptor agonist
Short-acting
Used as an anesthetic especially for CV surgery
Used pre-operatively for sedative, anxiolytic & analgesic effects
Used intra-operatively as adjunct or primary anesthetic
Term
Sufentanil
Definition
Synthetic opioid receptor agonist
Short-acting
Term
Remifentanil
Definition
Synthetic opioid receptor agonist
Short-acting, most potent
Term
Pentazocine
Definition
Mixed opioid receptor agonist/antagonist
Agonist activity >> antagonist activity
Term
Buprenorphine
Definition
Mixed opioid receptor agonist/antagonist
Partial activation of mu receptors
Term
Naloxone
Definition
Opioid receptor antagonist
Used to treat opioid dependence
Reverses opioid overdose
No activation of mu, delta or kappa receptors
Term
Naltrexone
Definition
Opioid receptor antagonist
Used to treat alcohol dependence
No activation of mu, delta or kappa receptors
Term
Loperamide
Definition
Opioid receptor agonist
Used to treat diarrhea
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