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Block 1
Pharm Flashcards- Block 1
65
Pharmacology
Graduate
01/21/2010

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Term
What are the positive sx of Schizophrenia? Why do these sx occur?
Definition
Delusions, hallucincations, bizarre behavior, disorganized speech and thinking and insomnia. Occur bc of excessive neuronal activity.
Term
First drugs (2) of choice for Schizophrenia
Definition
Reserpine and chlorpromazine
Term
What are the negative sx of Schizophrenia?
Definition
Withdrawl, lack of motivation, affective flattening, anhedonia avolution/apathy
Term
Characteristics of Schizophrenia
Definition
Characterized by a marked thinking disturbance, genetically linked, assoc with DA
Term
Where is the highest concentration of dopamine receptors?
Definition
Caudate nucleus
Term
What is significant about the caudate nucleus?
Definition
Involved in motor functions and has been shown to be atrophic in pts with Parkinson's Dz
Term
Projects from cell bodies near the substantia nigra to the limbic system.
Definition
Mesolimbic-Mesocortical (Dopaminergic System)
Term
Projects from the substantia nigra to the caudate and putamen (involved in voluntary movements).
Definition
Nigrostriatal (Dopaminergic System)
Term
Connects arcuate nuclei and perventricular neurons to the hypothalamus and posterior pituitary (DA released by these neurons inhibits PRL secretion)
Definition
Tubero-infundibular (Dopaminergic System)
Term
Neurons in the motor nucleus of the vagus whose projections are not well defined (involved in eating behavior)
Definition
Medullary-Periventricular (Dopaminergic System)
Term
Connects the medial zone incerta to the hypothalamus and the amygdala.
Definition
Incerto-hypothalamic (Dopaminergic System)
Term
What are the role of DA Antagonists?
Definition
Block dopamine in the mesolimbic and mesocortical systems (mainly at the D2 receptor). They produce antipsychotic effects and parkinsonian-like sx
Term
How do you manage an individual with Schizophrenia?
Definition
Hospitalization, Group therapy, Individual psychotherapy, meds, ET (Electroconvulsive therapy)
Term
What are the goals of Pharmacologic Mgt in a pt with Schizophrenia?
Definition
Control behavior, calm agitation, psychomotor slowing (decreased agitation, aggression and impulsivity)
Term
Schizophrenia pts who are resistant to pharmacotherapy tend to have...?
Definition
Negative sx
Term
What are the 4 main groups of Antipsychotic Agents?
Definition
1. Phenothiazine derivatives
2. Thioxanthene derivatives
3. Butyrphenone derivatives
4. Atypical (more effective with negative sx)
Term
How many days does it take to decrease the sx assoc with Schizophrenia?
Definition
3-10 days (Doses should be reduced gradually to a maintenance level)
Term
A contraindication of phenothiazine is?
Definition
Alcohol
Term
Antipsychotic Agents are indicated in what type of disorders?
Definition
1. Schizophrenia (primary indication)
2. Schizoaffective disorder
3. Psychoses assoc with depression and mania
4. Manic phase in bipolar affective disorder
5. Tourette's Syndrome
6. Alzheimer's Dz
7. Antiemetic
8. Pruritus (Phenothiazines-H1 blocking)
9. Preoperative sedatives (Promethazine)
Term
Prochlorperazine and Benzquinamide are used for as what? And what do they do?
Definition
Antiemetic. They block the DA receptor in the chemoreceptor trigger zone of the medulla and peripherally in the stomach.
Term
Antipsychotics are NOT indicated for...?
Definition
Withdrawl sx.
Term
Phenothiazine derivatives affect what type of receptors?
Definition
DA, muscarinic, H1, 5-HT2 (located throughout the CNS, autonomic and endocrine systems)
Term
Examples of Phenothiazine derivatives are?
Definition
1. Chloropromazine
2. Thioridazine
3. Piperazine (more potent, more selective)- exs: trifluoperazine, perpherazine, fluphenazine
Term
Haloperidol is a type of...?
Definition
Butyprophenone Derivative (Most widely used). It is more potent and has fewer autonomic effects but greater extrapyramidal effects.
Term
Atypical antipsychotics inhibit what type of receptors?
Definition
5-HT2 and DA2 (both with similar potency)
Term
Examples of Atypical Antipsychotic Agents are (6)?
Definition
1. Clozapine (limited to those who have failed conventional drugs, SE: agranuloctosis, seizure)
2. Olanzapine
3. Quetiapine
4. Risperidone
5. Ziprasidone
6. Aripiprazole
Term
The following describes what type of drug class? Readily but incompletely absorbed; significant first pass metabolism; highly lipid soluble and protein bound (Longer duration of action, full relapse may not be seen until 6 wks after discontinuation of drugs)
Definition
Antipsychotics
Term
What are some behavioral SE due to Antipsychotics?
Definition
1. Pseudodepression- due to drug induced akinesia (responds to antiparkinson drugs)
2. Confusion
Term
What are some neurologic effects (Extrapyramidal) due to administration of Antipsychotics?
Definition
Parkinson's Syndrome, akathisia, acute dystonic rxns, tardive dyskinesia, seizures
Term
How do you tx pts who have developed tardive diskinesia from taking antipsychotics?
Definition
1. Dose reduction or d/c offending agents
2. Eliminate all anticholinergic drugs, esp antiparkinsonism and TCAs
3. Switch to atypical
4. Diazepam 30-40 mg/day
5. May subside within 1 yr
Term
What are common CV SE from using typical antipsychotics? What are the MC drugs that cause these SE?
Definition
Postural hypotension, prolongation of QTc interval (may lead to V. arrhythmia).
Thioridazine and pimozide
Term
The MC SE of Fluphenazine, Clozapine and Olanzapine is?
Definition
Wt gain
Term
The MC SE's (2) of Chlorpromazine and Thioridazine are?
Definition
Seizures and retinal pigmentation
Term
1. MC SE from using Phenothiazines? 2. Other SE include?
Definition
1. Photosensitivity, rash and uticaria
2. Orthostatic hypotension, high resting HR
Term
The only antipsychotic that causes retinal deposits (browning of the vision)?
Definition
Thioridazine
Term
Ziprasidne has the greatest risk of?
Definition
QT prolongation (avoid combination with thioridazine, pimozide, quinidine)
Term
This syndrome is seen in 1% of pts on antipsychotics. It is MC with use of typical antipsychotics and is life threatening.
Definition
Neuroleptic Malignant Syndrome
Term
S/S of Neuroleptic Malignant Syndrome include?
Definition
Marked muscle rigidity (muscle relaxants such as dantrolene may help), fever, altered BP, increased pulse rate and WBC, elevated CK, severe extrapyramidal syndrome follows (tx with antiparkinsonism drugs)
Term
Extrapyramidal syndromes are a SE of Phenothiazine derivatives. Examples of these are:
Definition
Acute dystonic rxns: torticollis-neck, opisthotonos back and oculogyric crises- mouth and eye
Term
Drug-induced parkinsonism is a SE of Phenothiazine derivatives. Examples of these are? Tx?
Definition
cogwheel rigidity, bradykinesia, tremor, mask-like faces, drooling and loss of postural reflexes. Tx: antiparkinsonian meds like benztropine (cogentin) and trihexyphenidyl (artane)
Term
What is akathisia?
Definition
(Phenothiazine derivative SE) Motor restlessness syndrome, involves the entire body
Term
Tardive dyskinesia is a SE of Phenothiazine derivatives. What is it? It's characterized by?
Definition
Movement disorder, due to DA-AChl imbalances. Characterized by fasciculations, twisting and protrusion of the tongue, lateral jaw movements, lip smacking, 7 choreoathetotic movements of the extremities and trunk; reversed by neuroleptic discontinuation, irreversible in severe cases; worsen by the use of anticholinergic meds
Term
Overdoses of antipsychotics are ___________? Sxs include:
Definition
RARELY fatal (except mesoridazine and thioridazine). SX: drowsiness, coma, agitation, neuromuscular excitablity, convulsions, miotic pupils, DTR are decreased, hypotension and hypothermia.
Term
This is often referred to as an "antimanic" drug but in many parts of the world known as "mood-stabilizing" agent.
Definition
Lithium Carbonate (Eskalith)
Term
Lithium is FORMLY known as the drug of choice for tx of:
Definition
Mania, manic episodes of bipolar disorders and prevent mood swings in bipolar affective disorder
Term
The bipolar affective disorder is characterized by:
Definition
Mood swings, strong familial component and a mania phase (grandiosity, bellicosity, paranoid thoughts, overactivity)
Term
MOA of lithium (3):
Definition
1. Generates AP
2. Effects on NTs: 5-HT, NE, DA (decreases NE and DA turnover which might be relevant to antimanic action)
3. Effects on 2nd messengers and intracellular enzymes the mediate transmitter action (most promising)
Term
Lithium Absorption? Excretion? 1/2 life? Target plasma concentration? Dosage?
Definition
6-8 hrs, peak 30 min- 2 hrs
mainly in urine
20-24 hrs
0.6-1.4 mEq/I
0.5 mRq/kg/day in divided doses
Term
Valproate, olanzapine, atypical antipsychotics replaced ____________ in order to tx bipolar affective disorder
Definition
Lithium bc lithium has a slow onset of action (10-14 days).
Term
Recurrent endogenous depression can be controlled by?
Definition
lithium or imipramine
Term
Schizoaffective disorder is treated with?
Definition
Antipsychotic drugs alone or in combo with lithium
Term
When should the 1st concentration of lithium be obtained after the start of tx?
When should serum lithium concentrations be drawn after the last dose?
Definition
5 days. 10-12 hrs.
Term
Does lithium have a narrow or wide therapeutic index? Maintenance levels? Toxic levels?
Definition
NARROW! Maintenance levels: 0.9 mEq/L (0.6-1.2)
Toxic >2.0
Term
Lithium use reduces renal clearance by 25% when used with?
Definition
Diuretics (thiazides) and NSAIDs (asa and acetaminophen do NOT interact)
Term
ALL neuroleptics except _____ and _____ exhibit more severe EPS when combined with lithium.
Definition
clozapine and atypicals
Term
Adverse effects of lithium include:
Definition
tremor (alleviated by propranolol and atenolol), choreoathetosis, motor hyperactivity, ataxia, dysarthria, asphasia. At TOXIC level- mental confusion and withdrawl (stop lithium and closely monitor)
Term
Decreased thyroid fxn is a major SE of Lithium. What affects does lithium have on the thyroid? How often should TSH be monitored?
Definition
Lithium is distributed mostly in brain and thyroid. Blocks thyroid hormone synthesis and release. Reversible and nonprogressive. Monitor every 6-12 months!
Term
Common renal SE of lithium use include? Tx?
Definition
polyuria, polydipsia (common and reversible); nephrogenic diabetes insipidus (resistant to vasopressin but responds to amiloride); chronic interstitial nephritis and minimal change glomerulopathy with nephrotic syndrome.
Tx: well hydrated, periodic renal testing
Term
Edema, Bradycardia-tachcardia ("sick sinus") syndrome, transient acneiform eruptions, folliculitis and leukocytosis are SE of?
Definition
Lithium use
Term
What do you do when a pt overdoses on Lithium?
Definition
Plasma concentration may not be excessively high (2+is indicative of toxicity), dialyzed readily (peritoneal dialysis, hemodialysis*), continue dialysis until the plasma concentration falls below the usual therapeutic range.
Term
Can Lithium be used during prego?
Definition
Yes. Close level monitoring after delivery is important (levels will be expected to decrease)
Term
Can Lithium be used during prego?
Definition
Yes. Close level monitoring after delivery is important (levels will be expected to decrease)
Term
Can Lithium pass through breast milk?
Definition
Yes. Passes through with a concentration of about 1/3 to 1/2 of serum
Term
What are the S/S of newborn toxicity?
Definition
Lethargy, cyanosis, poor suck, moro reflexes, hepatomegaly
Term
Drugs for the depression phase of bipolar include?
Definition
1. TCA-linked to precipitation of mania, with more rapid cycling of mood swings
2. SSRIs- less likely to induce mania
3. Bupropion- induce mania at higher doses
4. Lamotrigine- effective for many pts with biopolar depression
5. MAO-I
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