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61 Cards in this Set
- Front
- Back
- 3rd side (hint)
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What class of antidepressants do Imipramine (trofanil), Amitriptyline (elavil) andd.doxepin (Sinequan) belong to?
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tricyclic antidepressants
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What is the method of action of tricyclics? Block NE, DA, Serotonin
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Block NE, DA, and Serotonin
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Are the tricyclics effective in reducing depression and anxiety?
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Yes, they work at least as well as the SSRIs and Benzodiazapines
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Why aren't tricylics used more now?
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The lethal dose is only 4-10x the effective dose, so it was a risk with the suicidal; also they have strong anticholingeric effects and made people uncomfortable. Anticholinergic effects also reduced cognition. The antihistamine in them caused sedation
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Does imipramine have an approved use in children?
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Yes, for bedwetting. Therefore imipramine was used for ADHD because it had a safety record in children. However, there is QT elongation and EKGs are required.
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What two antidepressants combine effects on NE and serotonin?
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Venlafaxine and duoloxetine (Effexor and Cymbalta)
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Is Cymbalta approved for neuropathic pain?
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yes
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What is the advantage of a combination antidepressant?
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It works on depression through two known pathways---NE leading to increased energy and concentration and Serotonin leading to reduced anxiety and depression.
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a. What is the method of action of buproprion (Welbutrin
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It is a DA transport blocker and weak NE blocker with little or no 5HT action
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What are the uses of buproprion?
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It avoids side effects of SSRIs and can add a new mechanism of action when added to SSRI. It is also used as an aid to quitting smoking
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Who should avoid buproprion?
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Individuals with seizure disorder and alcoholics (who could have seizures)
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How do trazodone and mirtazapine work (Deseryl and Remeron)
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Both of these increase serotonin through novel means (not by blocking reuptake). They can be used as adjuncts to SSRIs to boost serotonin. They also both have strong antihistamine actions so they are used to induce sleep
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There are 5 SSRIs. What are they?
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Sertaline (zoloft)Fluoxetine (Prozac) Citalopram (Celexa) Escitalopram (Lexapro)Paroxetine (Paxil)
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fluvoxamine is also an SSRI but its used primarily for OCD
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What is SSRI method of action?
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Block serotonin presynaptic autoreceptors, which increases serotonin, leading to decrease in postsynaptic receptors and possible release of brain derived neurotropic factor
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What are approved uses of SSRIs?
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Adult depression, anxiety, panic disorder, PTSD, OCD, eating disorders
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Why is there a black box warning for children with SSRIs?
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Increased suicidal ideation has been found. Also SSRIs are not as effective in children as in adults
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What are negative effects of SSRIs?
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Initial increase in anxiety, sexual dysfunction, nausea, sometimes sleep disturbance
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Can SSRIs induce mania?
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yes
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What is serotonin syndrome?
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A rare syndrome of excessive serotonin with autonomic lability, GI upset, agitation, Hyper/hypotension
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What is MAO
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monoamine oxidase -an enzyme that decomposes serotonin, NE and dopamine in the neuron.
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So inhibiting MAO does what?
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Allows more NE, Serotonin,and DA to be reused, thus starting a cascade that can reduce depression and anxiety
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Why are MAOI’s rarely used?
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There is a risk for a fatal reaction if an individual eats certain hard cheese, hard sausages, or red wines that contain TYRAMINE. The dietary restrictions scare prescribers and patients
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Is Lithium still a first line drug for mood stabilization?
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Yes, it is quite effective but does cause tremor and diarrhea and weight gain
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Why do we monitor Lithium levels?
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Lithium is lethal in small overdose
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Which other drug classes are used for mood stabilization?
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The anticonvulsants that work on NA or CA channels or GABA reuptake, plus those that work to reduce glutamate. Most anticonvulsants affect cognition adversely and cause weight gain. Atypical antipsychotics are often used as monotherapies but concerns about metabolic syndrome are problematic.
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Are the anticonvulsants FDA approved for mood stabilization?
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Carbamazapine is in its long acting form called Equetro.
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Which anticonvulsants have negative effects on cognition?
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All have some negative effects on cognition. Phenobarbital and Topiramate may be the worst.
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How do the anticonvulsants work?
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Most reduce neural excitation by reducing CA or NA channel transmission. Lamotrigine reduces glutamate; Tiagabine inhibits GABA reuptake, Topiramate havs multiple methods of action.
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What is the method of action of the “typical” antipsychotics?
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D2 receptor inhibition (in all DA pathways when we only want it in mesolimbic)
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How are the atypicals different from the typicals?
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They also inhibit Serotonin 2 receptors. The interaction between Serotonin and Dopamine allow more Dopamine in nirostriatal and tuberofundibular pathways and also in mesocortical pathway, which improves negative symptoms while still maintaining D2 blockage in mesolimbic
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What causes Extra Pyramidal Symptoms?
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DA/Ach imbalances in nigrostriatal pathways.
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What is Tardive Dyskinesia-
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a response to chronic DA blockade. Gait, limb, and buccal/tongue movements are affected. It is not always reversible when the medicine is discontinued.
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What is Neuroleptic Malignant Syndrome?
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A rare but potentially fatal reaction with hyperthermia, and muscle rigidity
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What are side effects of typical antipsychotics?
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Those with little Ach effect (like Haldol) can cause EPS. Almost all are sedating, reduce cognitive speed and cognitive efficiency
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What are side effects of typical antipsychotics with Ach action (like Thorazine) –
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cognitive blunting, constipation, hypotension, weight gain
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What are side effects of atypicals?
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Metabolic syndrome, increased risk for diabetes, stroke in the elderly
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Which antipsychotic is recommended for Parkinson’s patients?
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Quetiapine (seroquel)
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What fatal side effect is associated with Clozapine?
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Agranulocytosis
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What method of administration is recommended for noncompliant psychotic patients?
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Depot Haldol or Risperdal Consta
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Do benzodiazapines aid cognition?
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No, they reduce memory; some can be used to induce short term anterograde amnesia
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b. What is the drug of choice for preventing seizures during alcohol withdrawal
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Ativan, Serax or Librium
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What is the method of action of benzodiazapines?
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When GABA binds to a Chloride channel, stimultaneous binding of benzodiazepine will keep allow more Chloride to enter
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What other substances bind to the same receptor?
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Alcohol and Barbiturates
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e. All benzodiazepines will cause physical dependence at regular doses within 2-8 weeks. TRUE or FALSE?
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true
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Which of these is not a form of methylphenidate?
Adderall Metadate Concerta Straterra |
Adderall and Straterra. Adderall is a mix of amphetamine. Straterra increases NE rather than focusing on DA. It is closer to a tricyclic antidepressant than to methylphenidate.
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Stimulants are controlled substances TRUE OR FALSE
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TRUE
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What is the method of action of the stimulants?
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Indirect facilitation of NE and DA
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What are common side effects of Ritalin?
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Sleep onset delays, slowing of weight gain, anxiety, potentiation of tics
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What is modafinil?
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It improves alertness and concentration and promotres wakeful attention. Trade name is Provigil. It will have a different trade name when marketed for ADHD.
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What is the method of action of Aricept?
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It inhibits the enzyme Achetylcholinesterase which breaks down Achetylcholine., thus increasing Ach in the synapse
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What is the method of action of Namenda?
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It’s in the name: NMDA antagonism
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What improvement can be expected with the cognitive enhancing drugs?
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6-12 months delay of decline
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What does ADME mean in pharmacokinetics?
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Absorption, distribution, metabolism and excretion---this is what the BODY does to the DRUG
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Drugs that are bound to albumin are not available for active use by the body TRUE OR FALSE
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TRUE
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Drugs reach steady state in the body after what length of time?
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3.3 half lives. This is also how long it takes for a drug to wash-out of the body after discontinuation
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Ambien has been implicated in deaths from drowsy morning driving TRUE or FALSE
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TRUE
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Ambien has been implicated in uncontrolled middle of the night eating TRUE OR FALSE
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TRUE
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Sonata has a much shorter half life than the other non-benzodiazapine sleep aids TRUE OR FALSE
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TRUE--it shortens sleep latency
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Ambien, Sonata, and Lunesta are not benzodiazapines. TRUE OR FALSE
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true-but they do work at similar receptors at BZ 1 receptors only
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Older individuals need lower dosages of drugs because
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Their kidneys may be declining and they do not excrete drugs as quickly, so more drug stays in the body
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What is the method of action for Namenda in dementia tx?
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Namenda reduces the disintegration of neurons.
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