Neuropsych Drugs Part 2 Flashcards
What are symptoms of manic bipolar disorder?
Increased talkativeness, Increased distraction, inflated self-esteem, racing thoughts
How does Lithium work?
Lithium prevents the recycling of IP2 back to inositol, essentially stopping the secondary messenging causing manic symptoms.
(IP3 is the active substrate)
What is Lithium primarily used for?
Treating Mania, preventing recurrent bipolar disease, and cluster headaches
What are unique characteristics of Lithium?
There is a narrow therapeutic window and is effected by sodium levels. Diuretics can cause lithium levels to increase due to excretion of sodium. Also with ACE/ANGII inhibitors.
What are side effects of Lithium?
Early side effects - fatigue, weakness, ataxia, GI symptoms
Toxicity - impaired consciousness, rigidity, and hyper-reflexive. Contraindicated in pregnancy.
Need to regularly monitor levels
What can be used as an alternative to Lithium?
Carbamazepine
How does Carbamazepine work?
They both block sodium channel by inhibiting repetitive action potentials
Why is Lithium first line therapy over Carbamazepine?
Carbamazepine, induces cytochromes and has unpredictable absorption. Dose dependant sedation, diplopia, ataxia, and GI symptoms. Tetragenic
- More side effects and interactions -
What is primarily used to prevent seizures?
Valproic Acid and Divalproex
How do Valproic Acid and Divalproex work?
Inhibits repeative firing of APs via sodium channels, increased concentration of GABA and reduces Ca+2 currents. (Increases threshold for seizure)
What are symptoms of general anxiety disorder?
Symptoms persistent for 1 month. ANS stimulation - tachy, jittery, dry mouth, sweaty, nervous.
What are the type of neurotransmitters present during the major phases of sleep?
Slow wave - Serotonin
REM Sleep - Norepinephrine
How do benzodiazepines work?
They bind to the BDZ binding site on GABA receptors causing MORE FREQUENT and INCREASED binding of GABA. Causing inhibition - hyperpolarization
–Enhances GABA Action–
What is an antagonist to Benzodiazepines?
Flumazenil
What is a non-benzodiazepine that can be used for anxiety disorder?
Buspirone
Binds 5HT1A receptors agonist
Less sedating - alternative to benzodiazepines
What are the three benzodiazepines used to treat anxiety?
Diazepam, Lorazepam, and Alprazolam
What are the differences between Diazepam and Lorazepam?
Diazepam - more lipophilic, fast onset, rapid redistribution, short acting, and has active metabolite with fluctuating half life (can build up with repeative doses)
Lorazepam - slower onet, slow absorbance/redistribution, longer acting, No active metabolites
What benzodiazepine has the metabolite oxazepam?
Diazepam - the metabolite is still active and can cause increased side effects as repeat doses
What are side effects of benzodiazepines?
Decreases CNS effects, lowers anxiety, increases sedation, anticonvulsant.
Minimal CV and Respiratory effects
Amnesia after IV administration– used with sedation
What can happen if benzodiazepines are used with other CNS depressors?
If taken with ethanol or antihistamines can cause additive effects of each other.
What are the most common uses for benzodiazepines?
Anxiety, sleep disorder, muscle relaxants, seizure treatment, alcohol withdraw, and sedation/anesthesia
What is key when stopping the use of benzodiazepines?
You should gradually reduce the dose and switch to long acting drugs.
Benzodiazepines can cause dependence - opposite of their effects, anxiety, insomina, irritability, HA, hallucinations, seizures
What are the three benzodiazepine hypnotic agents?
Flurazepam, Triazolam, and Lorazepam
How do the benzodiazepines affect sleep?
Decrease threshold to sleep, increases stage 1/2 sleep and Decreases stage 3/4 and REM sleep.
Rebound insomnia upon withdrawal
Side effects of benzodiazepine hypnotic agents?
Daytime sedation, dependence forming, rebound insomnia, ataxia, INCREASES DEATH RATE
What is a nonbenzodiazepine hypnotic agent?
Zolpidem. Binds BDZ receptor on GABA, but stage 3/4 and REM sleep are Less effected
What are the effects of barbiturates?
CNS Sedation, hyperpolarization, anticonvulsion, RESPIRATORY depression, tolerance, dependence
What can happen if there is abrupt stopping of barbiturates? or taking too much?
CNS symptoms including agitation, tremor, insomnia, and life threatening seizures.
Acute toxicity can cause respiratory depression, coma, and stupor
What is a barbiturate hypnotic agent?
Pentobarbital - also used for anti-convulsion
What is another hypnotic agent used in older people that has a pungent taste?
Chloral Hydrate - less effects on sleep stages than benzo/barb and has similar effects to barbiturates.
What is the benzodiazepine used for muscle relaxant?
Diazepam - binds GABA in the spinal cord reducing tone
What muscle relaxant interferes with Glu release from presynaptic neurons binding at GABA-B?
Baclofen - GABA analog binding to GABA-B causing hyperpolarization of the presynaptic neuron, limiting excitatory release. Less sedation than diazepam
What muscle relaxant binds at Alpha2 receptors?
Tizanidine - agonizes alpha2 preventing NE release, can cause drowsiness and hypotension
