L16: Pharmacotherapy Flashcards
(165 cards)
1
Q
A
2
Q
Dopamine Pathways
A
3
Q
Classification of AntiPsychotic Drugs
A
3
Q
what are synonyms of AntiPsychotic Drugs?
A
- Neuroleptic drugs.
- Anti-schizophrenic drugs.
- Major tranquilizers.
- Dopamine receptor antagonists.
4
Q
what does low potency mean?
A
Needs high dose to reach the therapeutic effect.
5
Q
Form of most AntiPsychotic Drugs
A
tablets (others may also be injectable e.g. Haloperidol)
6
Q
Compare Between Typical Antipsychotics and Atypical Antipsychotics in terms of:
- Mechanism
- Effect
- Excretion of drug
- Discontinuation
- Metabolic SE
- Prolactin
- Extrapyramidal SE
A
6
Q
MOA of AntiPsychotics
A
7
Q
Therapeutic Uses (indicatios) of AntiPsychotics
A
8
Q
Pharmacological Effects of AntiPsychotics
A
8
Q
Precaustions of using Antipsychotics
A
8
Q
Aspects of Adverse effects of Antipsychotics
A
- CNS
- ANS
- GIT
- Skin & Eye
- CVS
- Hematologic
- Endocrine
- Extrapyramidal
- NMS
8
Q
CI of AntiPsychotics
A
These drugs are contraindicated in:
1. Hypersensitivity
2. CNS depression
3. Blood dyscrasias
4. Parkinson’s disease
5. Liver, renal, or cardiac insufficiency
9
Q
CNS Adverse effects of Antipsychotics
A
9
Q
Results of anti-histaminic activity of antipsychotics
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- Sedation
- Weight gain
10
Q
ANS Adverse effects of Antipsychotics
A
11
Q
GIT Adverse effects of Antipsychotics
A
- Nausea
- Gl upset
11
Q
Skin & Eye Adverse effects of Antipsychotics
A
11
Q
CVS Adverse effects of Antipsychotics
A
- Hypotension due to a adrenergic blocking action
- Reflex tachycardia & arrythmia
- ECG: Q-T prolongation and T wave suppression
12
Q
Hematologic Adverse effects of Antipsychotics
A
Agranulocytosis - associated with: Clozapine (order CBC for follow up)
13
Q
Endocrine Adverse effects of Antipsychotics
A
14
Q
Symptoms of Pseudo-parkinsonism
A
tremor, shuffling gait, drooling, rigidity
15
Q
EPS effects of Antipsychotics
A
- Pseudo-parkinsonism
- Akinesia
- Akathisia
- Dystonia
- Oculogyric crisis
- Tardive dyskinesia
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Q
TTT of Pseudo-parkinsonism
A
Anticholinergics
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Symptoms of Akinesia
muscular weakness
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Symptoms of Akathisia
continuous restlessness and fidgeting
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TTT of Akathisia
Propranolol / Benzodiazepine
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Symptoms of Dystonia
involuntary Painful Sustained muscular movements [spasms] of face, arms, legs, and neck
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TTT of Dystonia
- Anticholinergic injection / Benzodiazepines
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Def of Oculogyric crisis
uncontrolled rolling back of the
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TTT of Oculogyric crisis
Oral Anticholinergic
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Def of Tardive dyskinesia
Abnormal Choreoathetoid writhing movements of the tongue, face, and body
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Incidence of Tardive dyskinesia
More common in women and after at least 6 months of treatment
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Prognosis of Tardive dyskinesia
Rarely reversible
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TTT of Tardive dyskinesia
substitute atypical antipsychotic agent, e.g.: CLOZAPINE
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Symptoms of Neuroleptic malignant syndrome
- Severe parkinsonian muscle rigidity
- Hyperpyrexia up to 107° f
- Tachycardia, Tachypnea, Fluctuations in blood
pressure, Diaphoresis
- Rapid deterioration of mental status
- Stupor and coma
- Lab shows: elevated liver renal function, myoglobin, WBC, CPK
- Mortality Rate 20%
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TTT of Neuroleptic malignant syndrome
1. Stop Antipsychotic Medications (first step in management)
2. Adjust general conditions (adequate fluids & vital signs)
3. Specific agents: Dantrolene (muscle relaxant), Bromocriptine (Dopaminergic Agonist)
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Evolution of Extra Pyramidal Symptoms (EPS) side effects
* 4 hours acute dystonia (muscle spasm, stiffness, oculogyric crisis)
* 4 days akinesia (parkinsonian symptoms)
* 4 weeks akathisia (restlessness)
* 4 months Tardive dyskinesia
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SE of Olanzapine /Clozapine
May cause significant weight gain.
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SE of Chlorpromazine
Corneal deposits
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SE of Thioridazine
Retinal deposits.
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SE of Risperidone
One of atypical antipsychotics causing hyperprolactinemia and EPS
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SE of Aripiprazole
Commonly cause akathisia
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Characters of Clozapine
- Usually used in: Resistant schizophrenia & Tardive dyskinesia
- Has antisuicidal effect
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SE of Clozapine
Side effects:
* Agranulocytosis (requires weakly WBC monitoring)
* Myocarditis
* Risk of seizure (if more than 300mg)
* Hypersalivation
* Metabolic syndrome
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Def of **Mood Stabilizing Agents**
Any medication that is able to decrease vulnerability to subsequent episodes of mania or depression; and not exacerbate the current episode or maintenance phase of treatment.
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Classification of **Mood Stabilizing Agents**
**Antimanic:** Lithium carbonate
**Anticonvulsants:** Carbamazepine, Clonazepam, Valproic acid, Lamotrigine, Gabapentin & Topiramate
**Antipsychotics (atypical)**
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MOA of **Lithium Carbonate**
Exact mechanism is unknown, however it probably works by:
1. Accelerating presynaptic reuptake and destruction of catecholamine.
2. Inhibiting the release of catecholamine
3. Decreasing postsynaptic serotonin receptor sensitivity
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indication of **Lithium Carbonate**
- Acute mania
- Prophylaxis for bipolar and unipolar mood disorder
- Schizoaffective disorder
- Cyclothymia
- Impulsivity and aggression
- Others like: bulimia nervosa, trichotillomania, cluster headache, borderline personality disorder.
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Dosage of **Lithium Carbonate**
900-2100 mg in 2-3 divided dose.
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Blood Lithium levels of **Lithium Carbonate**
- Therapeutic level 0.8-1.2 mEq/litre
- Prophylactic level 0.6-1.2 mEq/litre
- Toxic lithium level >1.5-2 mEq/litre
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CI & precautions of **Lithium Carbonate**
1. Hypersensitivity
2. Cardiac or renal disease
3. Dehydration
4. Sodium depletion
5. Brain damage
6. Pregnancy and lactation.
7. Caution with thyroid disorders, diabetes, urinary retention, history of seizures, and with the elderly
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SE of **Lithium Carbonate**
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Lithium Toxicity
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Symptoms at serum levels of lithium 1.5 to 2.0 mEq/L
* Blurred vision
* Ataxia
* Tinnitus
* Persistent nausea and vomiting
* Severe diarrhea
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Symptoms at serum levels of lithium 2.0 to 3.5 mE/L
- Excessive output of dilute urine
- Increasing tremors
- Muscular irritability
- psychomotor retardation
- Mental confusion
- Giddiness
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Symptoms at serum levels of lithium ≥ 3.5 mEq/L
- Impaired consciousness
- Nystagmus
- Seizures
- Coma
- Oliguria/ anuria
- Arrhythmia
- Myocardial infarction
- Cardiovascular collapse
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Nursing management to avoid side effects of lithium
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What are anticonvulsants used in mood managment?
1. Carbamazpine
2. Valproic Acid
3. Lamotrigine
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Indications of Carbamazepine
Especially useful in:
1. treating mania with mixed features
2. rapid-cycling bipolar disorder
* Less effective for the depressed phase.
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Monitoring in Carbamazepine
CBC and LFTs must be obtained before initiating treatment and regularly monitored during treatment
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MOA of Carbamazepine
- Acts by blocking sodium channels and inhibiting action potentials. (exact mechanism is unknown)
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osnet of Carbamazepine
Onset of action Is 5-7 days (quicker than lithium)
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SE of Carbamazepine
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MOA of Valproic acid
Multiple mechanisms of action:
1. Blocks sodium channels
2. Increases GABA concentrations in the brain.
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Indications of Valproic acid
Useful in treating acute mania, mania with mixed features, and rapid cycling.
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Monitoring of Valproic acid
CBC and LFTs must be obtained before initiating treatment and regularly monitored during treatment
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Therapeutic level of Valproic acid
- Therapeutic range is 50-150 pg/mL.
- Drug levels should be checked after 4-5 days.
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SE of Valproic acid
Care should be given in women of childbearing age as it is:
1. Contraindicated in pregnancy (cause neural tube defects).
2. Causes:
Polycystic ovary (PCO)
Weight gain
Alopecia
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MOA of Lamotrigine
Believed to work on sodium channels that modulate glutamate and aspartate.
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Indication of Lamotrigine
Efficacy for bipolar depression, though little efficacy for acute mania or prevention of mania.
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SE of Lamotrigine
- **Most common side effects** are dizziness, sedation, headaches, and ataxia.
- **Most serious side effect** is Stevens-Johnson syndrome (life-threatening)
- Rash involving skin and mucous membranes in 0.1 %, This is most likely in the first 2-8 weeks, but is minimized by starting with low doses and increasing slowly.
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Effects of valproate & lamotrigine on each other
- Valproate will increase lamotrigine levels
- Lamotrigine will decrease valproate levels
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what are anti-suicidal drugs?
lithium - clozapine
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Introduction to **Antidepressants**
- Used in many psychiatric disorders other than Depression.
- Full clinical response in 6-8 weeks in major depression, up to 6/12 weeks in obsessive compulsive disorder (OCD).
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Indications of **Antidepressants**
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Phases of TTT of **Antidepressants**
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Categories of **Typical Antidepressants**
- MAOI
- TCA
- SSRI
- SNRI
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Examples of **Monoamine oxidase (MAO) inhibitors**
Phenelzine
Tranylcypromine
Selegiline (selective MAO-B inhibitor)
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MOA of Monoamine oxidase (MAO) inhibitors
- Nonselective MAO inhibition, Increase levels of amine neurotransmitters
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Indications of **Monoamine oxidase (MAO) inhibitors**
1. Atypical depression
2. Anxiety
3. Hypochondriasis
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MOA of **TCA**
Block reuptake of NE and serotonin
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SE of **Monoamine oxidase (MAO) inhibitors**
- Hypertensive crisis with tyramine ingestion (in many foods, such as wine and cheese) and CNS stimulants (ß agonists, pseudoephedrine)
- Contraindicated with SSRIs or Meperidine [To prevent serotonin syndrome].
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Types of **TCA**
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Uses of **TCA**
1. Major depression
2. Bed wetting (imipramine)
3. OCD (clomipramine)
4. Fibromyalgia
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SE of **TCA**
- Sedation, alpha blocking effects.
- Atropine-like (anticholinergic) side effects: tachycardia, urinary retention.
- Tertiary TCAs (amitriptyline) have more anticholinergic effects than the secondary TCAs (nortriptyline).
- Desipramine is the least sedating and has lower Seizure threshold
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Toxicity of **TCA**
- 3Cs: Convulsions, Coma, Cardiotoxicity (arrhythmias).
- Respiratory depression, hyperpyrexia.
- Confusion and hallucination in elderly due to anticholinergic side effects [use nortriptyline].
**Treatment: NaHCO3 for CV toxicity.**
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Examples of **SSRIs**
Fluoxetine
Paroxetine
Sertraline
Citalopram
Escitalopram
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MOA of SSRIs
- Serotonin-specific reuptake inhibitors.
- Normally takes 2 weeks for antidepressants lo have an effect.
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Indications of **SSRIs**
1. Depression
2. OCD
3. Eating disorders
4. Social phobias
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SE of SSRIs
- Fewer than TCAs
- Gl distress, diarrhea
- Sexual dysfunction (anorgasmia)
- Serotonin syndrome
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Serotonin syndrome
- "Serotonin syndrome" with any drug that that increase serotonin (e.g.MAO inhibitors), symptoms are:
1. Hyperthermia, muscle rigidity
2. Cardiovascular collapse
3. Flushing
4. Seizures
**Treatment of Serotonin Syndrome: cyproheptadine (5-HT, receptor antagonist)**
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MOA of **SNRIs**
Venlafaxine
Duloxetine
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Examples of **SNRIs**
Inhibit serotonin and NE reuptake.
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Indications of **SNRIs**
1. Depression.
2. Venlafaxine is also used in generalized anxiety disorder
3. Duloxetine is also indicated for diabetic peripheral neuropathies
4. Duloxetine has greater effect on NE
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SE of **SNRIs**
- Increase BP most common
- stimulant effects
- Sedation
- Nausea
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what are atypical antidepressants?
- Trazodone
- Bupropion
- Mirtazapine (NaSSA)
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MOA of **Trazodone**
Primarily inhibits serotonin reuptake.
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Indications of Trazodone
insomnia, As high doses are needed for antidepressant effects.
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# Toxicity of
Toxicity of Trazodone
sedation, nausea, priapism, postural hypotension. **vip**
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MOA of **Bupropion**
Inhibits DA and NA uptake has excitant effect
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Uses of Bupropion
- reduce smoking
- Approved for resistant and Bipolar depression
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SE of Bupropion
No sexual Side effect
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Toxicity of Bupropion
stimulant effects (tachycardia, insomnia), headache, seizure in bulimic patients.
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MOA of **Mirtazapine (NaSSA)**
- Noradrenergic and specific serotonergic antidepressant
- Block a2 adrenergic antagonist (increase release of NE and serotonin) potent 5-HT2 and 5-HT receptor antagonist.
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Toxicity of **Mirtazapine (NaSSA)**
No Sexual or Git side effects
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SE of Mirtazapine (NaSSA)
sedation, increase appetite, weight gain, dry mouth
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Indications of **Anti-Anxiety Drugs**
1. Generalized Anxiety (GAD)
2. Post-Traumatic Stress Disorder (PTSD)
3. Phobias
4. Obsessive Compulsive Disorder (OCD)
5. Panic Disorder
6. Insomnia related to Anxiety
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Classification of **Anti-Anxiety Drugs**
- Barbiturates
- Benzodiazepines
- Non barbiturates and non benzodiazepines
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Uses of **Benzodiazepines**
- Benzodiazepines are considered CNS depressants.
- They are used to produce sedation, induce sleep, relieve anxiety and muscle spasms, and to prevent seizures
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MOA of **Benzodiazepines**
- Enhance the actions of the neurotransmitter, GABA, which slows down brain activity.
- This produces a drowsy or calming affect
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SE of **Benzodiazepines**
- Drowsiness, dizziness, loss of coordination, fatigue, mental slowing, confusion.
- Withdrawal reactions are possible, 5/S: anxiety, shakiness, headache, dizziness, seizures.
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CI of **Benzodiazepines**
Acute narrow angle glaucoma
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Precautions while using **Benzodiazepines**
* With elderly
* Lung disease
* Liver disease
* Kidney disease
* Sleep apnea
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Safety Concerns while using **Benzodiazepines**
- Risk of addiction: should be only used short term.
- Patient should not drive or operate heavy machinery.
- Not to be mixed with ETOH, opiates, OTC cough/allergy medications, dental anesthetics - can be life threatening (resp, depression)
- MUST NOT be discontinued abruptly (Taper schedule is prescribed).
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Classification of **Benzodiazepines**
- Long Acting (Half-life: >20 Hours)
- Intermediate Acting (Half-Life: 6- 20 Hours)
- Short Acting (Half-life:<6 Hours)
- Very short half-life
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Half-Life of **Long Acting Benzos**
- more than 20 hours
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Examples & Uses of **Long Acting Benzos**
**Diazepam (Valium):** Rapid onset, Effective for muscle spasm, Less commonly prescribed to treat anxiety because of euphoria
**Clonazepam (Klonopin):** Avoid with renal dysfunction.
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Half-Life of **Intermediate Acting Benzos**
Between 6 & 20 Hours
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Half-Life of **Short Acting Benzos**
Less than 6 Hours
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Examples & Uses of **Intermediate Acting Benzos**
**Alprazolam (Xanax):** Treatment of anxiety, including panic attacks
**Lorazepam (Ativan):** Treatment of panic attacks, alcohol and sedative-hypnotic-anxiolytic detoxification, agitation. Not metabolized by liver
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Uses of **Very Short Acting Benzos**
Primarily used in medical and surgical settings
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Examples & Uses of **Short Acting Benzos**
**Triazolam (Halcion):** Treatment of insomnia.
- Risk of anterograde amnesia and sleep-related activities (e.g., eating, driving)
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Examples of Non-Benzo Anxiolytics
- Buspirone (BuSpar)
- Z-agents
- Antihypertensives acting on autonomic nervous system
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Characters of **Buspirone (BuSpar)**
- In contrast to BZs, buspirone is nonsedating and is
not associated with dependence, addiction, or withdrawal
- It is used primarily to treat conditions causing chronic anxiety, in which BZ dependence can become a problem (e.g., generalized anxiety disorder)
- Buspirone takes up to 2 weeks to work
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what are Z-Agents?
- Zolpidem (Ambien)
- zaleplon (Sonata)
- eszopicione (Lunesta)
- ramelteon (Rozerem)
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Characters of **Z-Agents**
- are short-acting agents
- used primarily to treat insomnia.
- Z-agents act on the GABA Receptor
- In contrast, ramelteon is a selective melatonin
ramelteon (Rozerem) agonist.
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Characters of **ramelteon**
ramelteon is a selective melatonin agonist.
121
Examples of **Antihypertensives acting on autonomic nervous system**
- beta blockers (block both a-1 and ß-2 adrenergic receptors) propranolol (Inderal)
- a-2 adrenergic receptor antagonists such as clonidine (Catapres)
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Actions of Antihypertensives acting on autonomic nervous system
decrease autonomic hyperarousal and are used to treat symptoms of anxiety (e.g., tachycardia), particularly in patients with social anxiety.
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Uses of **Psychostimulants**
Used in ADHD, Narcolepsy and in treatment of refractory depression.
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Examples of **Psychostimulants**
- Dextroamphetamine and amphetamines (Dexedrine, Adderall)
- Methylphenidate (Ritalin, Concerta)
- Atomoxetine (Strattera)
- Modafinil (Provigil)
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Characters of **Dextroamphetamine and amphetamines (Dexedrine, Adderall)**
..
126
Characters of **Methylphenidate (Ritalin, Concerta)**
..
127
Characters of **Atomoxetine
(Strattera)**
..
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Characters of **Modafinil (Provigil)**
Used in narcolepsy, not ADHD
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Drugs for Alcohol withdrawal
Benzodiazepines
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Drugs for Anorexia/bulimia
SSRIs
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Drugs for Anxiety
* Benzodiazepines
* Buspirone
* SSRIs
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Drugs for ADHD
* Methylphenidate (Ritalin)
* Amphetamines (Dexedrine)
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Drugs for Atypical Depression
* MAO inhibitors
* SSRIs
134
Drugs for Bipolar
"Mood stabilizers":
* Lithium
* Valproic acid
* Carbamazepine
* Atypical antipsychotics
135
Drugs for Depression
* SSRIs
* SNRIs
* TCAS
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Drugs for Depression with insomnia
Mirtazapine
137
Drugs for OCD
* SSRIs
* Clomipramine
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Drugs for PTSD
SSRIs
139
Drugs for Panic Disorder
* SSRIs
* TCAs
* Benzodiazepine
140
Drugs for Schizophrenia
Antipsychotics
141
Drugs for Tourette Symdrome
Antipsychotics (haloperidol)
142
Drugs for Social Phobias
SSRIs
143
Steps of **ECT**
1. Patients are often premedicated with atropine, and then given general anesthesia (typically with methohexital) and muscle relaxants (e.g., succinylcholine).
2. A generalized tonic-clonic seizure is then induced using unilateral or bilateral electrodes.
**While the mechanism of action of ECT is not fully known, there are likely anticonvulsant effects, as well as brain perfusion and connectivity changes involved.**
144
Indications of **ECT**
1. ECT is the most effective treatment for major depressive disorder, especially with psychotic features, as well as for acute mania and catatonia.
2. It is often used in patients who cannot tolerate medications or who have failed other treatments.
145
Duration of **ECT**
* ECT is discontinued after symptomatic improvement, typically a course of 8-12 sessions given three times weekly.
146
Monthly maintenance ECT is often used to prevent ....
relapse of symptoms.
147
SE of **ECT**
The most common side effects are:
- muscle soreness, headaches, amnesia ,and confusion. Bilateral electrode placement is more efficacious, but I memory impairment and confusion.
148
What is **DBS**?
- DBS is a surgical treatment involving the implantation of a medical device that sends electrical impulses to specific parts of the brain.
149
Uses of **DBS**
DBS in select brain regions has provided benefits for Parkinson's disease and disabling dystonia, as well as for chronic pain and tremors.
150
Mechanism of **DBS**
Its underlying principles and mechanisms are still not clear.
151
Indications of **DBS** in Psychiatry
DBS has been used to treat various affective disorders, including major depression.
152
Effect of **DBS**
DBS directly changes brain activity in a controlled manner and its effects are reversible (unlike those of lesioning techniques).
153
what is **Repetitive transcranial magnetic stimulation (rTMS)**?
rTMS is a noninvasive method to excite neurons in the brain.
154
,.
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SE of **Repetitive transcranial magnetic stimulation (rTMS)**
include seizures (rare), as well as headache and scalp pain.
156
Characters of **Repetitive transcranial magnetic stimulation (rTMS)**
- Weak electric currents are induced in the tissue by rapidly changing magnetic fields, a process called electromagnetic induction.
- In this way, brain activity can be triggered with minimal discomfort.
- rTMS can produce longer-lasting changes than nonrepetitive stimulation.
- Numerous small-scale studies have demonstrated efficacy in the treatment of major depression; however, studies show less efficacy than for ECT, and the price of treatment is high
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