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Pharmacology - Final - Part 12

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davidwurbel7's version from 2016-08-14 06:57

Parkinson's Disease

Question Answer
A degenerative disorder of the CNS that often impairs the sufferer's motor skills and speech. Symptoms include Tremor at rest, Rigidity, Bradykinesia / akinesia: respectively, slowness or absence of movement, Postural instability, Gait abnormalities, fatigue and Soft speech/droolingParkinson's Disease
D2 receptor antagonists (antipscychoics) that can lead to Parkinsonian symptoms even at therapeutic levelsHaloperidol
A chemical which destructs the dopaminergic neurons leading to irreversible parkinsonismMPTP
An antimuscurinic drug that decreases cholinergic activity in drug inducted parkinsonismBenztropine
Most effective drug for parkinsonian symptoms. Immediate precursor of dopamine, does enter the brainLevodopa
Levodopa is converted to dopamine by this enzymeDOPA-decarboxylase
The other name for DOPA-decarboxylaseAromatic L-amino acid Decarboxylase
A drug inhibiting peripheral DOPA-DecarboxylaseCarbidopa
A dopamine preparation containing carbidopa and levodopa in fixed proportion (1:10 or 1:4)Sinemet
The advantages of this drug are more amount of L-dopa available in brain; a lower doses of L-dopa can be used lessening the peripheral effects of dopamineSinemet
When this drug is given alone it can cause anorexia and nausea and vomiting occurLevodopa
A variety of cardiac arrhythmias, including tachycardia, ventricular extrasystoles and, rarely, atrial fibrillationLevodopa
Dyskinesias occur in up to 80% of patients receiving long term therapy of this drug (chorea, ballism). Choreoathetosis of face and distal extremitiesLevodopa
Occurrence of involuntary movements in a combination of chorea and athetosisChoreoathetosis
A continuous stream of slow, sinuous, writhing movements, typically of the hands and feet. It is said to be caused by damage to the corpus striatum of the brainAthetosis
Quick movements of the feet or hands are vaguely comparable to dancing or piano playingChorea
Serious, slight movements will become thrashing motions, this form of severe choreaBallism
Behavioral adverse effects a wide variety of adverse mental effects have including depression, anxiety, hallucinations, and other changes in mood or personalityLevodopa
Alternating effects in which symptoms are well controlled and when symptoms are not well controlledOn-Off Phenomenon
This drug enhances the extracerebral metabolism of levodopa and may therefore prevent its therapeutic effectPyridoxine
Levodopa is contraindicated in patients with this condition as levodopa may exacerbate mental disturbancePsychosis
Levodopa is contraindicated in patients with this condition as it may increase the intraocular pressure due to dilation of the pupilGlaucoma
Levodopa is contraindicated in patients with this condition since it is a precursor to melaninMalignant Melanoma
Acts as a partial agonist at D2 receptors in the brainBromocriptine
Acts as an agonist at D2 receptors in the brainPergolide
Agonist at D3 receptors, now considered first line drugs, less ADRPramipexole
This drug is also used for treatment of hyperprolactinemia & acromegalyBromocriptine
Both Bromocriptine and pergolide are contraindicated for patients with thisPsychosis
Increased amounts of dopamine in the mesolimbic and mesocortical regions of the brain can lead to thisPsychosis
An increase in the levels of dopamine will decrease the levels of this hormoneProlactin
Selegiline and rasagiline inhibit this enzymeMonoamine Oxidase-B
Entacapone and tolcapone inhibit this enzymeCatechol-O-Methyltransferase (COMT)
MAO-B is the isoform that metabolizes this in preference to NE and 5-HTDopamine
Adverse effect include insomia, mood changes, GI distress and hypotensionMAO Inhibitors
Drug interaction of MAO inhibitors with this drug that can cause agitation, delirium & deathMeperidine
Extreme caution with TCA and SSRI due to serotonin syndrome with interaction with this drugMAO Inhibitors
Increased plasma levels of this indicates poor response to Levodopa3-O-Methyldopa
This drug inhibits COMT in both central and peripheralTolcapone
This drug inhibits COMT in only the peripheralEntacapone
An adverse effect of this drug is hepatic damageTolcapone
The preferred COMT inhibitor is due to no hepatic toxcityEntacapone
The proposed mechanism of action is increased synthesis, release and inhibition of dopamine reuptake. It is less efficacious than levodopa, and its benefits may be short-lived, often disappearing after only a few weeks of treatmentAmantadine
Adverse effects include restlessness, depression, irritability, insomnia, agitation, excitement, hallucinations, and confusionAmantadine
Benztropine, biperiden, procyclidine & trihexyphenidyl are this class of drugAnticholinergic (Antimuscurinic)
This class of drugs is used to treat drug-induced parkinsonismAnticholinergic (Antimuscurinic)
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Question Answer
Propranolol – b-blocker Also can use topiramate (anti-epileptics)Tremors
Tetrabenazine, reserpine – depletes cerebral dopamine and HaloperidolHuntington’s Chorea
For multiple tics - Haloperidol (blocks central D2 R) and also carbamazepine, clonazepam and clonidine (a2 agonist)Tourette’s Syndrome
Treated with chelator – penicillamineWilson’s Disease
DA agonist – ropinirole or pramipexoleRestless Leg Syndrome
Prochlorperazine can be used to treatEmesis
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Antipsychotic Drugs

Question Answer
Typical antipsychotic agents block these receptors, and their binding affinity is very strongly correlated with clinical antipsychotic and extrapyramidal potencyD2 Receptors
Atypical antipsychotic drugs(clozapine, olanzapine) are effective at lower occupancy levels of 30–50%, because of their concurrent high occupancy of this receptor5-HT2A Receptors
Increased dopamine levels in the mesolimbic pathway result inPositive Symptoms
Decreased dopaminergic activity in mesocortical pathway result inNegative Symptoms
Symptoms hallucination, delusions, thought dysfunction are these type of symptoms in schizophreniaPositive Symptoms
Symptoms such as deficiencies in emotional responsiveness, spontaneous speech and volition, flattening of affect, poverty of speech, and drive, loss of feeling, social withdrawal and decreased spontaneous movementNegative Symptoms
Typical antipsychotic Drugs (D2 receptor antagonist) that include chlorpromazine, fluphenazine, thioridazine, trifluoperazinePhenothiazines
Typical antipsychotic Drug (D2 receptor antagonist) that is not a PhenothiazineHaloperidol
Clozapine, asenapine, olanzapine, quetiapine, risperidone, sertindole, ziprasidone, zotepine, and aripiprazole are examples of this class of antipsychoticsAtypical Drugs
These are treated by benztropine, biperiden, trihexphenyl, diphenhydramineExtra Pyramidal Symptoms
Acute Dystonia (spastic retrocolis or torticolis), Akathisias (motor restlessness) and Parkinson-like symptoms (tremors, bradykinesia, rigidity) are these types of symptomsExtra Pyramidal Symptoms
Hyperprolactinemia is treated with thisBromocriptine
An increase in the levels of Dopamine will cause a decrease in the levels of thisProlactin
Late occurring side effect of antipsychotics with oral/facial dyskinesias, muscle jerks, writhing of lip musclesTardive Dyskinesias
Tardive Dyskinesias is treated by thisSwitching to an Atypical Antipsychotic
Initial symptoms is marked muscle rigidity, alterations in BP and HR, hyperthermia. Muscle-type creatine kinase elevatedNeuroleptic malignant syndrome (NMS)
Neuroleptic malignant syndrome (NMS) is treated with thisDantroline
Neuroleptic malignant syndrome (NMS) with muscle tremors is treated with Dantroline and thisDiazepam
Weight gain which is very common with clozapine and olanzapine due to thisH1 Receptor Blockade
A side effect seen with this drug is agranulocytosis which requires weekly blood countsClozapine
A side effect seen with this drug is retinal deposit- browning of vision and also ventricular arrhythmias due to prolong QT intervalThioridazine
The mechanism of action is to inhibit the recycling of PIP2-depletion of second messenger- DAG &IP3Lithium
The signs of toxicity include severe tremors (imp 1st sign of toxicity) drowsiness, ataxia, Nephrogenic diabetes insipidus, Benign reversible thyroid enlargement and rarely hypothyroidismLithium
This is the first sign of lithium toxicity in a patientSevere Tremors
Lithium is contraindicated in pregnancy due to thisEbstein's Anomaly
Nephrogenic diabetes insipidus due to lithium toxicity is treated with thisAmiloride
The mechanism of action inhibits the recycling of PIP2-depletion of second messenger- DAG &IP3. Has low therapeutic index, plasma levels has to be monitoredLithium
Drug of choice for bipolar disorderLithium
The therapeutic range of this drug is 0.5-1.4 mmol/lLithium
Toxicity signs include nausea, vomiting, diarrhea, fine tremors, polydipsia and Nephrogenic diabetes insipidusLithium
Treatment for nephrogenic diabetes insipidus that becomes unresponsive to ADHAmiloride
Drug of choice for nephrogenic diabetes insipidusDemopressin/Vasopressin
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Antidepressants

Question Answer
Fluoxetine, Fluvoxamine, Sertraline, Paroxetine, Citalopram and Escitalopram are examples of this class of drugsSSRIs
Inhibit serotonin transporter (SERT). They block only serotonin (not NE) reuptake leading to elevated serotonin levelsSSRIs
Serotonin and NE reuptake inhibition with effects on multiple receptor system (H1, M, and alpha 1) and sodium conductanceTCA
Inhibit serotonin and norepinenephrine transporters only without any effect on other receptorsSNRIs
Blocks 5-HT 2 receptors but also are weak SERT inhibitors5-HT 2 Antagonists
Tetracyclic and unicyclic antidepressantsAtypical Antidepressants
Inhibits the action of mono-amine oxidaseMAO-Inhibitors
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Question Answer
Fluoxetine is metabolized to this active formNorfluoxetine
This class of drugs are CYP inhibitorsSSRIs
Seen in up to 40% of all patients and is a reason for non compliance with SSRIsSexual Dysfunction
This SSRI is associated with weight gainParoxetine
Venlafaxine, Desvenlafaxine, Duloxetine are examples of this class of drugSNRIs
Amitriptyline, Desipramine, Doxepin, Imipramine, Nortriptyline, trimipramine, clomipramine and protriptyline are examples of this class of drugTricyclic Antidepressants (TCA)
Class of antidepressant drug class that lack the potent antihistamine, adrenergic blocking, and antimuscarinic effectsSNRIs
Class of antidepressant drug class that has potent antihistamine, adrenergic blocking, and antimuscarinic effectsTricyclic Antidepressants (TCA)
Antidepressant drug that has more affinity to bind to SERT than it does to NETClomipramine
Clomipramine can be used along with any SSRIs to treat thisOCD
Side effects include serotonergic A/E (diarrhea, vomiting) and noradrenergic effects- increase BP and HR, and CNS activation, such as insomnia, anxiety, and agitationSNRIs
Side effects include Alpha-1 Blockade: orthostatic hypotension, sexual dysfunction, cardiac conduction delays (QT prolongation), Histamine Blockade: weight gain, sedation, Anti cholinergic: Dry mouth, Blurred vision, constipation, urinary hesitancy, Sexual Dysfunction, Lowers seizure threshold – seizures may occurTricyclic Antidepressants (TCA)
Signs of overdoses of this class of drug include coma, convulsions, cardiac arrhythmiasTricyclic Antidepressants (TCA)
Treatment for TCA overdoseIV Sodium Bicarbonate
Trazadone and Nefazodone are examples of this class of drug5-HT2 Antagonists
This drug causes the adverse effects of mainly sedation and priapismTrazodone
5-HT2 Antagonist that inhibits CYP3A4Nefazodone
Nefazodone inhibits this enzymeCYP3A4
Bupropion, Amoxapine, Maprotiline and Mirtazapine are examples of the class of drugAtypical Antidepressants
Mechanism of action of this drug is increased NE and DA activity. no effect on 5-HT (No sexual dysfunction). Used for smoking cessationBupropion
This drug is contraindicated in persons with epilepsy as it lowers the seizure thresholdBupropion
These drugs NET > SERT inhibitionAmoxapine and Maprotiline
Mechanism of action of this drug is antagonism of presynaptic alpha2 receptors, increase release of NE, 5-HT . Also an antagonist of 5-HT2 and 5-HT3 and is a potent H1 antagonist (sedation)Mirtazapine
This drug antagonism of presynaptic alpha 2 receptor and increases release of NE and5-HT. Also an antagonist of 5-HT2 and 5-HT3 and is a potent H1 antagonistMirtazapine
This drug adverse effects are sedation and weight gainMirtazapine
Phenelzine and Tranylcypromine are examples of this class of drugNonselective MAO Inhibitors
Selegiline is an example of this class of drugSelective MAO –B Inhibitors
Treatment for cheese reaction is thisPhentolamine
The co-administration of SSRIs and MAO-Is may lead to thisSerotonin Syndrome
Clinical findings include Hyperthermia, Mental Status Changes, seizures, muscular rigidity, tremor, myoclonus, hyperreflexia and increased muscle creatine kinaseSerotonin Syndrome
The treatment for Serotonin Syndrome is thisDantrolene and Diazepam
A 5-HT 2 antagonist that can be used to treat Serotonin Syndrome in conjunction with diazepam and dantroleneCyproheptadine
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SSRIs, SNRIs, 5-HT antagonists, preferred over TCAs because of better tolerability
Bipolar disorder(for depressive phase) SSRI /TCAs in combination with Lithium (for maniac phase)
Panic disorder- SSRIs, venlafaxine
Obsessive compulsive disorder- clomipramine, SSRI(especially fluvoxamine)
Enuresis (bedwetting)- Imipramine
Attention deficit hyperactivity disorder(ADHD)- TCAs and Atomoxetine
Patients who want to withdraw from nicotine dependence(to quit smoking)- Bupropion
Neuropathic pain and fibromyalgia- Duloxetine, TCA
GAD , panic attacks, social phobias, post-traumatic stress disorder, bulimia, and premenstrual dysphoric disorder- SSRI

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