p.10
Clinical Overview of Parkinsonism
What is schizophrenia primarily characterized by?
A clear sensorium but marked thinking disturbance; considered a neurodevelopmental disorder.
p.9
Drug Interactions and Contraindications
Which drugs have less obvious interactions with sedative-hypnotics?
Antihypertensives, antihistamines, and antidepressants.
p.9
Clinical Pharmacology of Sedative-Hypnotics
What is Flumazenil's role in relation to GABA?
It is a competitive antagonist at the BZD binding site in the GABAA receptor.
p.11
Clinical Pharmacology of APD
Which antipsychotic is known for its antiemetic effects?
Most antipsychotics except thioridazine.
p.9
Clinical Pharmacology of Sedative-Hypnotics
What is the major metabolism process for barbiturates?
Oxidation by hepatic enzymes to form alcohols, acids, and ketones.
p.6
Clinical Pharmacology of Sedative-Hypnotics
What is the primary effect of sedatives?
They reduce anxiety and produce a calming effect.
p.10
Clinical Overview of Parkinsonism
What is psychosis characterized by?
A variety of mental disorders and grossly disorganized thinking in a clear sensorium.
p.6
Clinical Pharmacology of Sedative-Hypnotics
What structural feature is required for sedative-hypnotic activity in benzodiazepines?
A substituent in the 7th position, such as a halogen or nitro group.
p.9
Adverse Effects of Anti-Parkinson's Drugs
What are the side effects of Flumazenil?
Agitation, dizziness, nausea, confusion.
p.11
Pharmacologic Effects
Which pathway inhibits prolactin secretion?
Tuberoinfundibular pathway.
p.9
Clinical Pharmacology of Sedative-Hypnotics
Which sedative-hypnotics bind to the GABAA receptor?
Benzodiazepines, barbiturates, and newer sedative-hypnotics.
p.6
Clinical Pharmacology of Sedative-Hypnotics
How does lipophilicity affect the absorption of sedative-hypnotics?
It determines the rate at which a sedative-hypnotic enters the CNS.
p.10
Levodopa and its Pharmacokinetics
What effect does levodopa have on schizophrenia?
It aggravates schizophrenia or produces psychosis.
p.10
Pathophysiology of Parkinson's Disease
What is the role of the 5-HT2A receptor in the serotonin hypothesis?
Its stimulation is the basis for the hallucinatory effects of hallucinogens like LSD.
p.6
Clinical Pharmacology of Sedative-Hypnotics
What is a potential consequence of cumulative effects from benzodiazepines?
Patients may sleep excessively and have reduced activities due to accumulation of metabolites.
p.10
Adverse Effects of Anti-Parkinson's Drugs
What is a common side effect associated with older generation antipsychotics like haloperidol?
Extrapyramidal symptoms (EPS).
p.13
Clinical Overview of Parkinsonism
What are the symptoms of the depressive phase in bipolar disorder?
Anxiety, sleep disturbance, depressed mood, and high risk for suicide.
p.6
Clinical Pharmacology of Sedative-Hypnotics
What is the primary effect of hypnotics?
They produce drowsiness and encourage the onset and maintenance of sleep.
p.8
Clinical Pharmacology of Sedative-Hypnotics
What are some clinical uses of sedative-hypnotics?
Relief of anxiety, insomnia, sedation before procedures, treatment of epilepsy, and muscle relaxation.
p.12
Antipsychotic Agents and Lithium
What is the primary basis for choosing antipsychotic drugs?
Differences in adverse effects and efficacy.
What effect does alkalinization of urine have on phenobarbital?
It can greatly increase its elimination.
p.8
Adverse Effects of Anti-Parkinson's Drugs
What is cross-tolerance in the context of sedative-hypnotics?
Tolerance that develops between different sedative-hypnotics, including ethanol.
p.14
Dopamine Receptor Agonists
What does stimulation of the 5-HT2C receptor lead to?
Excitation of cortical and limbic dopamine release.
p.12
Antipsychotic Agents and Lithium
What is clozapine reserved for?
Patients who do not respond to conventional antipsychotic drugs.
p.2
Adverse Effects of Anti-Parkinson's Drugs
What cardiovascular issues can arise from levodopa treatment?
Arrhythmias, including tachycardia and postural hypotension.
What are the effects of thiopental and methohexital in anesthesia?
They penetrate brain tissue rapidly following IV administration.
p.12
Adverse Effects of Anti-Parkinson's Drugs
What is a rare but serious risk associated with thioridazine?
Ventricular arrhythmias and sudden death.
p.9
Drug Interactions and Contraindications
What types of drugs interact with sedative-hypnotics?
CNS depressants, alcohol, opioid analgesics, anticonvulsants, and phenothiazines.
p.11
Adverse Effects of Anti-Parkinson's Drugs
What adverse effect is associated with muscarinic cholinoceptor blockade?
Dry mouth, constipation, difficulty urinating, and orthostatic hypotension.
p.8
Adverse Effects of Anti-Parkinson's Drugs
What is a common side effect of prolonged use of benzodiazepines (BZD)?
Tolerance, leading to increased dosage requirements.
p.13
Adverse Effects of Anti-Parkinson's Drugs
What should be monitored every 6 months during lithium treatment?
Thyroid function (TSH levels).
p.10
Pathophysiology of Parkinson's Disease
What is the basis of the dopamine hypothesis in relation to schizophrenia?
Excessive dopamine activity plays a role in the disorder.
p.10
Dopamine Receptor Agonists
What is the main mechanism of action for clozapine and quetiapine?
They block the 5-HT2A receptor and act as inverse agonists.
How do BZDs affect GABAergic inhibition?
They potentiate GABAergic inhibition at all levels.
p.2
Clinical Overview of Parkinsonism
What is the best result timeframe for levodopa treatment?
Within the first year of treatment.
What is the role of flumazenil?
It is the drug of choice for reversal of BZD receptors.
p.12
Adverse Effects of Anti-Parkinson's Drugs
What are common metabolic and endocrine adverse effects of antipsychotic drugs?
Weight gain, hyperglycemia, hyperprolactinemia.
p.3
Catechol-O-Methyltransferase (COMT) Inhibitors
What is Stalevo a combination of?
Entacapone + Carbidopa + Levodopa.
p.11
Adverse Effects of Anti-Parkinson's Drugs
What is the mechanism behind tardive dyskinesia?
Dopamine receptor blockade.
p.12
Antipsychotic Agents and Lithium
Which generation of antipsychotic drugs is more effective for treating negative symptoms?
Newer antipsychotic drugs (APDs).
p.10
Pathophysiology of Parkinson's Disease
What does the glutamate hypothesis suggest about NMDA receptors?
Hypofunction of NMDA receptors on GABAergic interneurons contributes to schizophrenia.
p.3
Levodopa and its Pharmacokinetics
What is the starting dose for Pramipexole?
125 mcg or 0.125 mg 3 times daily.
p.10
Pharmacokinetics of Antipsychotic Agents
How are antipsychotic drugs metabolized?
Almost completely metabolized by oxidation or demethylation catalyzed by liver microsomal cytochrome P450 enzymes.
p.2
Drug Interactions and Contraindications
What is a 'drug holiday' in the context of Parkinson's treatment?
A period off medication for 3-21 days to improve responsiveness.
How do sedative-hypnotics affect respiration and cardiovascular function?
They can increase respiratory depression, especially in patients with pulmonary problems.
p.13
Clinical Overview of Parkinsonism
What are key symptoms of the manic phase in bipolar disorder?
Hyperactivity, impulsivity, aggression, disinhibition, decreased sleep, and cognitive impairment.
What is a common endocrine effect of older antipsychotic drugs in women?
Amenorrhea-galactorrhea and false positive pregnancy tests.
p.10
Pathophysiology of Parkinson's Disease
How do many antipsychotic drugs affect dopamine receptors?
They block the D2 receptor in the mesolimbic and striatal-frontal system.
p.3
Dopamine Receptor Agonists
What is the primary use of Pergolide?
Directly stimulates both D1 and D2 receptors.
What is the site of the BZD receptor on the GABAA receptor?
Between the alpha1 and gamma2 subunits.
p.12
Adverse Effects of Anti-Parkinson's Drugs
What are some neurological adverse effects of antipsychotic drugs?
EPS, akathisia, acute dystonic reactions, tardive dyskinesia, seizures.
p.2
Drug Interactions and Contraindications
What are some contraindications for levodopa treatment?
Psychotic patients, angle closure glaucoma, history of GI bleeding, suspicious skin lesions.
p.13
Levodopa and its Pharmacokinetics
How is lithium absorbed in the body?
Virtually complete within 6-8 hours, with peak plasma levels in 30 minutes to 2 hours.
p.13
Adverse Effects of Anti-Parkinson's Drugs
What are common neurologic adverse effects of lithium?
Tremors, seizures, confusion, ataxia, and dysarthria.
p.8
Adverse Effects of Anti-Parkinson's Drugs
What is physiological dependence?
An altered state requiring continuous drug administration to prevent withdrawal symptoms.
p.8
Adverse Effects of Anti-Parkinson's Drugs
What is Flumazenil used for?
It acts as a competitive antagonist at the BZD binding site in the GABAA receptor.
p.6
Clinical Pharmacology of Sedative-Hypnotics
What should be considered when prescribing sedative-hypnotics to the elderly?
Dosages should be reduced due to increased sensitivity and potential for prolonged effects.
p.8
Adverse Effects of Anti-Parkinson's Drugs
What is a significant withdrawal symptom from long-term use of sedative-hypnotics?
Severe anxiety and generalized seizures.
What is the primary action of barbiturates on GABA-gated chloride channels?
They increase the duration of channel openings.
p.3
Monoamine Oxidase Inhibitors (MAOIs)
What is the primary action of Rasagiline?
MAO B inhibitor and neuroprotective treatment.
p.2
Dopamine Receptor Agonists
What are the advantages of dopamine receptor agonists compared to levodopa?
No enzymatic conversion, no toxic metabolites, limited adverse effects.
p.9
Clinical Pharmacology of Sedative-Hypnotics
What are the clinical pharmacology indications for sedative-hypnotics?
Relief of anxiety, sedation and amnesia before procedures, treatment of epilepsy, and as a component of balanced anesthesia.
p.2
Levodopa and its Pharmacokinetics
How does levodopa enter the brain?
Via L-amino transporter (LAT).
p.6
Clinical Pharmacology of Sedative-Hypnotics
What is the metabolic pathway for benzodiazepines?
They undergo microsomal oxidation by cytochrome P450 isozymes and are conjugated to form glucuronides.
p.2
Levodopa and its Pharmacokinetics
What is the effect of carbidopa when combined with levodopa?
Reduces peripheral conversion of levodopa to dopamine, increasing availability to the brain.
p.12
Adverse Effects of Anti-Parkinson's Drugs
What are the side effects of clozapine?
Seizures and agranulocytosis.
p.2
Adverse Effects of Anti-Parkinson's Drugs
What is a common movement disorder associated with long-term levodopa treatment?
Dyskinesias, specifically choreoathetosis.
What are the anticonvulsant effects of phenobarbital and some BZDs?
They can be used to control seizures.
p.8
Adverse Effects of Anti-Parkinson's Drugs
What are the potential toxic effects of sedative-hypnotics?
CNS depression, anterograde amnesia, and exacerbation of breathing problems.
p.8
Adverse Effects of Anti-Parkinson's Drugs
What can happen with a lethal dose of sedative-hypnotics?
It can be fatal, with doses as low as 10 times the hypnotic dose being dangerous.
p.14
Dopamine Receptor Agonists
Which dopaminergic pathway is responsible for human behavior?
Mesolimbic-mesocortical pathway.
What are the three types of ligand interactions with BZD receptors?
Agonists, antagonists, and inverse agonists.
p.3
Monoamine Oxidase Inhibitors (MAOIs)
What is Selegiline's role in Parkinson's Disease treatment?
Adjunct treatment that enhances and prolongs the effect of levodopa.
p.3
Catechol-O-Methyltransferase (COMT) Inhibitors
What does the inhibition of COMT lead to?
Elevated levels of 3-0-methyldopa (3-0-MD) that competes with levodopa.
p.13
Clinical Pharmacology of Sedative-Hypnotics
What effect does lithium have on neurotransmitters?
Decreases norepinephrine and dopamine turnover, and augments acetylcholine synthesis.
p.11
Cardiovascular Effects
What cardiovascular effect is associated with phenothiazines?
Orthostatic hypotension and increased resting heart rates.
p.12
Adverse Effects of Anti-Parkinson's Drugs
What are the common adverse effects of older antipsychotic drugs?
Extrapyramidal symptoms (EPS) and hyperprolactinemia.
p.10
Clinical Pharmacology of Sedative-Hypnotics
What are the chemical types of antipsychotic agents?
Phenothiazine derivatives, thioxanthene derivatives, butyrophenone, miscellaneous structures, and atypical APD.
p.3
Dopamine Receptor Agonists
What is Ropinirole classified as?
Pure D2 receptor agonist.
p.2
Adverse Effects of Anti-Parkinson's Drugs
What are common gastrointestinal adverse effects of levodopa?
Anorexia, nausea, vomiting.
p.12
Adverse Effects of Anti-Parkinson's Drugs
What is the treatment approach for antipsychotic overdose?
Supportive measures and dialysis to increase drug elimination.
