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Pharmacology > Exam 3 Drug Situations > Flashcards

Exam 3 Drug Situations Flashcards

1
Q

This drug is a weak analgesic and muscle relaxant that causes CV/resp depression and sensitizes myocardium to catecholamines. Hepatic toxicity is seen

A

Halothane

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2
Q

This drug is a weak analgesic and muscle relaxant. It has CV depression and sensitizes myocardium to catecholamines. It is biotransformed with fluoride causing renal toxicity. A decreased threshold for seizures is seen. Contraindicated in labor

A

Enflurane

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3
Q

This drug has some transient resp stimulation. No catecholamine sensitization for myocardium.

A

Isoflurane

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4
Q

This drug has some transient resp stimulation. No catecholamine sensitization for myocardium. It has a very fast induction. It can react and form carbon monoxide.

A

Desoflurane

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5
Q

This drug is a good analgesic. It will present a second gas effect if used with another gas. It potentiates resp depression by other agents. It is a direct CV depressant.

A

Nitrous oxide

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6
Q

This drug is non-irritating with a sweet scent. It has a fast induction and emergence. Kids love it. There is significant renal toxicity.

A

Sevoflurane

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7
Q

This drug provides no analgesia of muscle relaxation. Resp and CV depression is seen. There is a reduction in intracranial pressure. Some patients have a reaction to it presenting as asthma, rashes, or acute intermittent porphyria. It works through a GABA enhancer role.

A

Ultra-short barbituates (Methohexital, thiopental, thiamylal)

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8
Q

This drug is water soluble with a short half life. It acts as a powerful amnestic. No analgesia of muscle relaxation seen. Its antidote is Flumazenil

A

Midazolam

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9
Q

This drug is highly abused. It is used as a dissociative anesthetic in which the patient is in a trance like state. Its mechanism is antagonism of NMDA receptor. Emergence is seen with excitement and hallucinations. This can be prevented with benzodiazepines. IM and IV routes provide similar pharmacology. There is an increase in intraocular and intracerebral pressures.

A

Ketamine

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10
Q

This drug provides no analgesia of muscle relaxation. It is painful when injected. You should not use it in stressed out patients as it may inhibit 11-beta-hydroxylase –> decreasing steroids for 24 hours.

A

Etomidate

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11
Q

This drug is the most commonly used anesthetic. It lowers blood pressure (avoid in CV or PV disease) and has a very low incidence of nausea and vomiting. It is great for outpatient surgery.

A

Propofol

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12
Q

These drugs are actually analgesics but used as an anesthetic. They are opiate agonists with short duration of action. They are used to aid induction and maintenance of general anesthesia. They are used with NO and droperidol to induce neuroleptanesthesia. Respiratory depression is longer than analgesia.

A

Fentanyl/Remifentanil

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13
Q

These drugs are used as a local anesthetic. They are preferred in pregnancy since they are hydrolyzed by pseudocholinesterase (very short half lives). Their final product is PABA which is antigenic. At high dose there is CNS stimulation. Medullary depression at high doses causes CV and Resp depression. Can be used topically, infiltratively, regional block, and spinal anesthesia.

Which is most common
Which lasts longer

A

Esters

Most common: Benzocaine
Longest acting: Tetracaine

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14
Q

These drugs are used as a local anesthetic. They are biotransformed by liver microsomal enzymes. They are allergy free. At high dose there is CNS stimulation. Medullary depression at high doses causes CV and Resp depression. Can be used topically, infiltratively, regional block, and spinal anesthesia.

Which is most common
Which lasts longer
Which has severe CV toxicity

A

Amides

Common: Lidocaine

Longest: Bupivacaine

CV toxic: Bupivacaine

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15
Q

Two drugs used for chronic anti-anxiety

A

SSRI’s

SNRI’s

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16
Q

These drugs work through GABA-A receptor enhancement. They are very lipid soluble. Used for anti-anxiety, sedation, anterograde amnesia, anticonvulsant, muscle relaxant, and in alcohol/CNS depressant tapering. They increase stage 2 sleep and decrease stage 3, 4, and REM sleep. There is toxic depression when combined with alcohol or other CNS depressants. Also interacts with P450 enzymes and has protein binding. Generally safe, there is a serious addiction and physical dependence issue. Abrupt discontinuation will result in life-threatening withdrawal. Paradoxical excitement and amnesia are seen. If overdose, flumazenil will reverse.

4 long acting
4 medium acting
2. short acting

A

Benzodiazepines

Long: Chlor, Clor, Dia, Flur

Medium: Lorazepam, Aprazolam, Temazepam, Estazolam

Short: Triazolam, Oxazepam

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17
Q

This drug is a partial agonist at serotonin 5-HT1A receptor for anti-anxiety. It has no tolerance, physical dependence or addiction. There are no interactions with ethanol or other CNS depressants. It has an interaction with monoamine oxidase inhibitors and will raise blodo pressure.

A

Buspirone

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18
Q

These drugs control the symptoms of anti-anxiety and are used with someone with test anxiety. They are non-selective usually.

A

Beta-blockers (propranolol most)

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19
Q

These drugs use their sedative effect to treat anxiety associated with anesthesia and surgery.

A

Anti-histamines

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20
Q

These drugs disrupt Stage 4 and REM for short-term treatment of insomnia. They are relatively safe. Oral form is preferred for sedation. It is an inhibitor of CYP2D6. Half life of 2-8 hours which will result in a drug hangover. Pregnancy class is type B. Reacts with alcohol/CNS depressants, anti-cholinergics, MAO-I’s, and OTC meds. Works through blockade of histamine-1 and cholinergic receptors.

A

Anti-histamines

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21
Q

This drug inhibits serotonin reuptake. It is used in patients that want restorative sleep but can’t be treated with benzodiazepines. Great for patients with depression or risk of substance abuse.

A

Trazodone

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22
Q

This pharmacon is used for insomnia, anxiety, and cramps. It works through prolonging GABA activity. Oral delivery with short duration. Avoid when pregnant or when taking other sedation, confusion causing drugs.

A

Valerian.

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23
Q

This drug is used to induce sleep. It is an agonist at melatonin 1 and 2 receptors. It is taken with a fatty meal. Drug hangover can occur in elderly patients. Pregnancy class C. Avoid in suicidal or sleep apena/COPD patients. Strage behaviors, memory, hallucinations and reduced sex drive are all common side effects. Interacts with CNS depressants. Bio-T Inhibitors are fluvoxamine and protease inhibitors. Inducers are anticonvulsants.

A

Ramelteon

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24
Q

This drug is for short term sleep induction or short term sleep maintenance. It does NOT affect REM or stage 4 sleep. Works through GABA-benzo complex at BZ1 or Omega1 subtype. Biotransformed by CYP3A4. Half life of 2.8 hours. Don’t use in patients with sleep apnea/COPD or are suicidal. Amnesia and withdrawal syndrome are seen. Anticholinergic side effects are seen. Interactions with CNS and hepatic enzymes are seen. Make sure to take when you are ready to sleep.

A

Zolpidem (Ambien)

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25
Q

This drug is for short term sleep induction. It does NOT affect REM or stage 4 sleep. Works through GABA-benzo complex at BZ1 or Omega1 subtype. Biotransformed by CYP3A4. Half life of 1 hour. Don’t use in patients with sleep apnea/COPD or are suicidal. Amnesia and withdrawal syndrome are seen. Interactions with CNS and hepatic enzymes are seen. Make sure to take when you are ready to sleep.

A

Zaleplon (Sonata)

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26
Q

This drug is for sleep induction and sleep maintenance and can be used long term. It does NOT affect REM or stage 4 sleep. Works through GABA-benzo complex at BZ1 or Omega1 subtype. Biotransformed by CYP3A4. Half life of 6 hours. Expect a drug hangover. Don’t use in patients with sleep apnea/COPD or are suicidal. Amnesia and withdrawal syndrome are seen. Interactions with CNS and hepatic enzymes are seen. Make sure to take when you are ready to sleep. Has anti-cholinergic, decreased libido, and increased risk of infections.

A

Eszopiclone (Lunesta)

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27
Q

These drugs hav ehigh abuse potential. They will suppress stage 3, 4, and REM while increasing stage 2. Bind to allosteric site on GABA. High likelihood of drug hangover. Biotransformed by CYP. Pregnancy category X due to side effects such as medullary depression and suicidal ideation and dependence. Withdrawal is life threatening. Do not use with alcohol or suicidal patients. Fluazenil is antiode for overdose

Which one is somewhat safe

A

Benzodiazepines (Estazolam, Flurazepam, Temazepam, Triazolam)

Temazepam probably safe in pregnancy

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28
Q

These drugs activate a GABA-allosteric site. They also block sodium channels at high doses. CNS, respiratory, and CV depression seen. 2 adverse reactions are CYP induction and physical dependence. If overdose, artificial respiration, purging of stomach, and hemodialysis is used.

Name the ultrashort acting
Name 3 short acting
Name one long acting

A

Barbituates

Ultra-short: Thiopental
Short: Pentobarbital, secobarbital, amobarbital,
Long: Phenobarbital

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29
Q

Three drugs for excessive daytime sleepiness of narcolepsy

A

Modafinil
Amphetamine
Methylphenidate

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30
Q

Two drugs for cataplexy

A

Fluoxetine

Selegiline

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31
Q

This drug is indicated for nacrolepsy, sleep apnea, shift work disorder (can’t stay awake), and fatigue with multiple sclerosis. Biotransformed by CYP3A4. Half life of 15 hours and is pregnancy category C. Acts like a stimulant. Interacts with MAO-I’s, CNS stimulants, and hepatic enzymes. Contraindicated in hepatic and renal failure patients.

A

Modafinil

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32
Q

Two drugs are indicated for narcolepsy and ADHD. Indirect and direct stimulation of NE and dopamine activity. Pregnancy category C. Adverse reactions include growth suppression, psychosis and depression, and DEPENDENCE which is a black box warning. Common adverse reaction includes Tics. Interacts with MAO-I, and CNS drugs. Should not be used in patients with epilepsy or CV or CBV disease.

A

Amphetamine and Methylphenidate

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33
Q

5 Sodium Channel Blockers

A 
PFCLF
Phenytoin
Fosphenytoin
Carbamazepine
Lamotrigine
Felbamate
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34
Q

This drug has a highly variable first pass effect. Typical side effects are nystagmus, ataxia, gingival hyperplasia, hirsutism, peripheral neuropathy. It is indicated for tonic-clonic, simple & complex partial seizures, and status epilepticus. Also indicated for cardiac arrhythmias. Do NOT use for absence or myoclonic epilepsy. Autoinducing drug. Generics are not recommended. Zero order kinetics when plasma levels are at or above therapeutic levels.

A

Phenytoin

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35
Q

This drug has a highly variable first pass effect. It is a prodrug with faster onset of action. Water soluble and given parenterally or intramuscularly. Has a high potential for drug-dispensing error. Typical side effects are nystagmus, ataxia, gingival hyperplasia, hirsutism, peripheral neuropathy. It is indicated for tonic-clonic, simple & complex partial seizures, and status epilepticus. Also indicated for cardiac arrhythmias. Do NOT use for absence or myoclonic epilepsy. Autoinducing drug. Generics are not recommended. Zero order kinetics when plasma levels are at or above therapeutic levels.

A

Fosphenytoin

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36
Q

This drug is indicated for partial seizures (Drug of choice) as well as tonic-clonic. Also used for mood stabilization in acute mania and bipolar and psychosis and migraines. It has toxic effects on liver, kidneys, and bone marrow. These must all be monitored.

A

Carbamazepine

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37
Q

This drug is the less toxic form of carbamazepine.

A

Oxcarbazepine

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38
Q

This drug acts similarly to phenytoin. It has less effect on p450 but Stevens-Johnson skin rashes and toxic epidermal necrolysis are seen.

A

Lamotrigine

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39
Q

This drug is similar to phenytoin. It also may block glutamate NMDA receptors. It is used when epilepsy is not responding to any other drugs. High incidence of aplastic anemia and Stevens-Johnson syndrome.

A

Felbamate

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40
Q

This anti-convulsant has slow absorption with low protein binding. Auto-induction likely. Mechanism is blockade of Na+ channels mainly. Excessive sedation, irritability, rash and blood dyscrasias all signify adverse reactions. Used in tonic-clonic, and partials. Do NOT use in absence or myoclonic epilepsy.

A

Phenobarbital

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41
Q

This anti-convulsant is biotransformed into phenobarbital and PEMA. A high ratio of this drug to phenobarbital suggests poor patient compliance with normally low phenobarbital accumulation. There is Na+ blocking along with GABA stimulation.

A

Primidone

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42
Q

This is probably the best drug for managing seizures. Has multiple actions including enhancing inhibition, blocking sodium channels, blocking calcium channels, and triggering hyperpolarization. Protein binding is near saturation which if saturation is hit, will result in zero order kinetics. Biotransformed product is hepatotoxic. Used for Tonic-clonic, partial, and Absence seizures. Also used for bipolar. Adverse effects include liver failure, alopecia, pancreatitis, red blood cell aplasias, teratogenicity. Interacts through bio-t, PB, and clonazepam which will result in status epilepticus or severe depression.

A

Valproic Acid

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43
Q

This drug acts similarly to valproic acid. It also blocks glutamate receptors and is a carbonic anhydrase inhibitor. It is indicated for partial and generalized seizures and treatment of migraines. Very few interactions.

A

Topiramate

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44
Q

These three drugs act by facilitating GABA inhibition and also block sodium channel activation. This is the only class that has developed tolerance to anti-epileptic activity

What are the three drugs and their indications.

A

Benzodiazepines

Diazepam: Status epilepticus

Lorazepam: Status epilepticus

Clonazepam: Atonic seizures, light sensitive seizures, myoclonic seizures, and infantile spasms

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45
Q

This is THE drug for absence epilepsy. It blocks T calcium currents and disrupts the spike and wave discharge. It is safe at normal doses but very toxic if too high.

A

Ethosuximide

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46
Q

This drug is indicated for partial seizures and blocks sodium channels as well as inhibits carbonic anhydrase. Orally active with a long half life. Adverse reactions include sulfonamide sensitivity.

A

Zonisamide

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47
Q

This drug is indicated for partial seizures. It slows inactivaiton of voltage-gated sodium channels. CV effects are seen.

A

Lacosamide

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48
Q

This drug inhibits GABA reuptake. It is indicated for partial seizures. It has a short half life that is challenging for dosing.

A

Tiagabine

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49
Q

This drug’s action is to inhibit kindling. It is used as an adjunct in partial, myoclonic and generalized seizures. Somnolence is seen when used in combos with other anti-seizures.

A

Levetiracetam

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50
Q

This drug is indicated for partial seizures. It is a potassium channel opener and GABA enhancer. Urinary retention and GI upset common.

A

Ezogabine

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51
Q

This drug works through calcium channels. Antacids decrease its absorption. It is used in partial seizures and Pain.

A

Gabapentin

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52
Q

This drug increases GABA synthesis. Indicated for pain and partial seizures.

A

Pregabalin

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53
Q

This drug inhibits carbonic anhydrase which promotes CO2 buildup which reduces sodium flux. Tolerance develops quickly so is quick acting. Used only in clearly defined periods of seizure vulnerability.

A

Acetazolamide

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54
Q

Vagal nerve stimulation is best for what

A

Partial seizures

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55
Q

Antileptics and pregnancy relationship

A

All are teratogenic

56
Q

4 main drugs for generalized seizures

2 alternatives

A

Valproic Acid, Carbamazepine, Phenytoin, Lamotrigine

Phenobarbital/primidone

57
Q

Absence seizure drugs (2)

1 alternative

A

Ethosuximide and Valproic acid

Clonazepam

58
Q

3 drugs for myoclonic seizures

A

Valproic acid, clonazepam, lamotrigine

59
Q

Status epilepticus drugs (4)

Alternative

A

IV diazepam or lorazepam, phenytoin, phenobarbital

General anesthesia

60
Q

These drugs were the first antidepressant. But they are really true antidepressants as they only mask the signs of depression. Acts as a stimulant

A

Amphetamines

61
Q

These drugs are the drugs of choice (first line) for depression. All are equally efficacious. GI upset, insomnia, anxiet, sexual dysfunction, weight loss, tremors and serotonin syndrome are all adverse effects. Withdrawal effects are noted. Black box warning for use in children and teenagers due to worsening the depression and suicide risk. Protein binding interaciton with digitoxin and cytochorme p450 are seen.

5 drugs specific drugs
Which are the same but one is racemic and one is S enantiomer

A

SSRI’s

Fluoxetine
Sertaline
Paroxetine
Fluvoxamine
Citalopram/Escitalopram

Citalopram is racemic and escitalopram is S-enantiomer which is 2X as potent.

62
Q

This SSRI is also used for pre-menstrual dysphoric syndrome. It is a long lived metabolite with half life of 8 days.

A

Fluoxetine

63
Q

These anti-depressants are second line drugs due to safety concerns. Dose dependent increase in blood pressure is common and severe withdrawal is noted for one of these drugs.

Name the two drugs. Which is more protein bound

A

SNRI’s

Venlafaxine
Duloxetine: Extensively protein bound

64
Q

Name 3 second generation drugs for depression

A

Bupropion
Trazodone
Nefazodone

65
Q

This drug blocks uptake of dopamine with little effect on NE or serotonin. There is little interaction with ethanol. There is a high incidence of seizures especially in patients with bulimia or when dose exceeds 450 mg/day. Incidence of psychosis. Also indicated for treating nicotine addiction.

A

Bupropion

66
Q

This drug is a blocker of the presynaptic serotonin receptor which promotes release. It has the side effects of priapism and hepatotoxicity.

A

Nefazodone

67
Q

This is the third generation drug that blocks presynaptic alpha-2 and serotonin-2 receptors to increase release of serotonin and norepinephrine. Used as an appetite enhancer and comes in quick dissolve tablet.

A

Mirtazapine

68
Q

These drugs block norepinephrine reuptake and some also block serotonin uptake. Indicated for long term treatment of depression and enuresis of childhood and pain. Weight gain and CV depressant effects as well. In overdose, acidosis occurs causing protein binding to decrase. Treat with alkalization through hyperventilation and sodium bicarbonate. Interacts with CNS depressants, sympathetic agents, MAO-I’s and anticholinergics. These are not drugs of choice. Narrow range between therapeutic blood levels.

A

Tricyclic Antidepressants

69
Q

This tricyclic blocks reuptake of both NE and serotonin

A

Imipramine

70
Q

This tricyclic is less sedating and less anticholinergic

A

Desipramine

71
Q

This tricyclic treats anxiety with depression. But AVOID in epileptics.

A

Maprotiline

72
Q

This tricyclic is approved for obessive-compulsive disorders.

A

Clomipramine

73
Q

This tricyclic has a serious sedative effect

A

Amitriptyline

74
Q

This tricyclic has low incidence of cardiac effects

A

Nortriptyline

75
Q

This tricyclic has sedation with no CV effects in healthy people. Do NOT use in CV disease patients.

A

Doxepin

76
Q

The long term effect is changes similar to those for tricyclics. Excessive CNS stimulation and sympathetic activity is seen. Interacts with any sympathetic drug or CNS drug. Also interacts with Meperidine and is contra-indicated with this. Indicated for long-term treatment of depression, narcolepsy. Kids and elderly should NOT use.
What are the two drugs

A

Monoamine-Oxidase inhibitors

Phenelzine and Tranylcypromine

77
Q

This MAO-I is an irreversible inhibitor of MAO. It has direct receptor agonist actions.

A

Tranylcypromine

78
Q

Two main SSRI’s used

A

Fluoxetine

Sertraline

79
Q

Two main SNRI’s used

A

Venlafaxine or Duloxetine

80
Q

One dopamine reuptake inhibitor

A

Bupropion

81
Q

Main two side effects of tricyclics

A

Orthostatic hypotension and cardiac problems

82
Q

Main side effect of bupropion

A

Seizures

83
Q

Main side effect of mirtazapine (2)

A

Weight gain and sedation

84
Q

Main two side effects of nefazodone

A

Sedation and drug-drug interactions

85
Q

Main side effect of traodone (3)

A

Sedation, dizziness, priapism

86
Q

SSRI main side effect

A

Sexual dysfunction

87
Q

MAO inhibitor main side effects (2)

A

Sexual dysfunction

Dietary concerns

88
Q

5 therapies for bipolar

A 
Lithium
Valproate
Anticonvulsants
Second generation antipsychotics
Electroconvulsive therapy
89
Q

How to treat mild manic or mixed episode of bipolar?

A

Lithium, valproate, second generation antipsychotic or anticonvulsant + short-term benzodiazepine
2 DRUGS

90
Q

How to treat moderate to severe mania or mixed episode

A

Lithium or valproate AND second generation antipsychotic agent + short term benzodiazepine
3 DRUGS

91
Q

How to treat mild to moderate depression in bipolar? 2

Alternative

A

Lithium or lamotrigine

Alternative anticonvulsants

92
Q

How to treat moderate to severe depression in bipolar?

A

Lithium or lamotrigine + antidepressant + second generation antipsychotic (3 DRUGS_

93
Q

This drug is used for classic bipolar. Pharmacokinetics are similar to sodium. 0.8 to 1.0 mEq/L is therapeutic range. Toxic episodes are result of sodium retention (dehydration). Interacts with diuretics, NSAID’s, and Anti-psychotics

A

Lithium

94
Q

3 drugs for classic bipolar?

A

Lithium
Valproate
Second generation anti-psychotics

95
Q

Two main medication sets for schizophrenia?

Which are typical?
Which are drugs of choice

A

Second generation agents (Atypical): Drugs of choice due to safety
First generation agents (Typical)

96
Q

Mechanism of actions of anti-psychotics?

A

Dopamine receptor blocking (D2 of mesolimbic)

Serotonin receptor blocking (5HT-2A)

97
Q

What are the 10 2nd generation atypical antipsychotics?

A 
Clozapine
Risperidone
Aripiprazole
Paliperidone
Olanzapine
Lurasidone
Asenapine

Ziprasidone
Iloperidone
Quetiapine

98
Q

This drug is a partial agonist at D2 and 5HT-1A by a strong antagonist at 5-HT2A receptors. 5 day half life. Indicated for schizophrenia and bipolar. Black box warning for dementia-related psychosis and suicidality. Metabolic syndrome seen.

A

Aripiprazole

99
Q

This drug blocks D1, D4, and 5-HT2 receptors. Does NOT block D2. High incidence of agranulocytosis is why its not first line anti-psychotic. Tardive dyskineasias, seizures, metabolic syndrome, weight gain are all seen.

A

Clozapine

100
Q

This might be second most effective antipsychotic. Weight gain and metabolic syndrome are still seen though. Akathisia and sedation seen. Also used for manic state of bipolar.

A

Olanzapine

101
Q

This atypical Anti-psychotic is an alpha-adrenergic blocker. Dise is titrated according to hypotensive effect. Cataracts seen in animals so you need to have an eye exam every 6 months.

A

Quetiapine

102
Q

This drug blocks D2 with high therapeutic doses and 5-HT2 at therapeutic doses. Likes to go to limbic structures. Some tardive dyskinesias seen. This is a first line antipsychotic.

A

Risperidone

103
Q

What is the active metabolite of risperidone

A

Paliperidone

104
Q

This anti-psychotic has QT prolongation and risk of sudden death. Do not use in patient with heart condition.

A

Ziprasidone

105
Q

This class of drugs has good efficacy for schizophrenia. Is better at treating negative and cognitive symptoms. Tardive dyskinesias which are irreversible motor problems have a low incidence. No effect on pro-lactin.

A

Atypical 2nd Gen Anti-psychotics

106
Q

These drugs have toxicity from muscarinic blockade, alpha-1 blockade, histmaine-1 blockade, and D2 blockade. Tardive dyskinesias and neuroleptic malignant syndrome are seen. Lipid soluble with hepatic biotransformation. They are indicated for psychosis, nausea and vomiting (except for one), intractable hiccough, Tourette’s, and Choreas. Poor safety record and limited patient benefit.

A

Typical 1st gen Anti-psychotics

107
Q

These drugs can be used to manage initial therapy of psychotic patients by reducing aggression, calming patient and allowing dose reduction.

A

benzodiazepines.

108
Q

What are the seven first generation anti-psychotics

A 
Alpiphatics: Chlorpromazine and Triflupromazine
Phenazine
Piperdines
Butyrophenones
Thioridazine
Thioxanthenes: Thiothixene
109
Q

Which 1st gen AP has high potency D2 antagonists and more extrapyramidal side effects

A

Triflupromazine

110
Q

Which 1st gen AP is a low potency D2 antagonists with NO anti-nausea effects

A

Thioridazine

111
Q

This first gen has a high incidence of extrapyramidal side effects and is the agent of choice for acute episodes of schizophrenia due to its powerful neuroepileptic effects.

A

Haloperidol

112
Q

This drug crosses the blood brain barrier using the aromatic acid transport system. Absorption is enhanced by takin gdrug on empty stomach or with low protein foods. It is converted to its active form in peripheral and central tissues. Iron oxidizes it, VItamin B6 increases its peripheral conversion. MAO-I’s and dopamine agonists interfere with its action. On-Off reactions are seen. Nausea, orthostatic hypotension, cardiac arrhythmias, anorexia, hallucinations, dyskinesias, and mental distrubrances are seen. Its active form in the central tissues enhances dopamine levels.

A

Levadopa

113
Q

This drug inhibits peripheral action of L-amino acid decarboxylase allowing more levadopa to cross the BBB. It reduces peripheral symptoms of dopamine.

A

Carbidopa

114
Q

This drug inhibits monoamine oxidase B which degrades dopamine in the brain. Its use increases central levels of dopamine in neurons. It is used in addition to levadopa therapy. Its intermediate is amphetamine. Meperidine is contraindicated and interactions with monoaminergic drugs are seen at higher doses.

A

Seligiline

115
Q

This drug is an irreversible inhibitor of MAO-B but has no amphetamine-like intermediates. Used in addition to L-dopa therapy. Meperidine and monoaminergic drug interactions are seen.

A

Rasagiline

116
Q

This drug is used as a peripheral inhibitor of COMT. It decreases peripheral conversion of dopa to enhance central uptake. It is used as an adjunct in levodopa/carbidopa therapy. Diarrhea and orange discoloration of urine is seen.

A

Entacapone

117
Q

This drug is used as a peripheral and central inhibitor of COMT. It decreases conversion of dopa to enhance its central uptake. It is used as an adjunct in levodopa/carbidopa therapy. Diarrhea and orange discoloration are seen. Hepatic necrosis is seen as well.

A

tolcapone

118
Q

This drug contains three doses of levodopa/carbidopa and one dose of entacapone. It can NOT be split. It saves money by combining all of the parts into one pill.

A

Stalevo

119
Q

This drug is a short duration amphetamine with dopamine agonist, anticholinergic, and NMDA receptor antagonist action. It is used for initial treatment of Parkinson’s or during levadopa drug holidays

A

Amantadine

120
Q

These drugs can only be used when L-DOPA is still beneficial. These are mainly centrally acting but if peripheral will cause hypotension, cardia arrhytmia, nausea and vomiting. Sudden sleep episodes and halucinations are also seen.

What are the four drugs

A

Direct Dopamine Agonists

Bromocriptine
Pramipexole
Ropinirole
Rotigotine

121
Q

This direct dopamine agonist is used as monotherapy or as an adjunct to L-DOPA. It has high tachyphylaxis and tolerance when used in monotherapy. It is also indicated for restless leg syndrome.

A

Rotigotine

122
Q

These Parkinson’s drugs work centrally mainly in order to reduce cholinergic tone. Peripheral side effects are still seen. Need drug holidays to keep the drugs in use due to tolerance.

What are the 3 drugs

A

Anti-cholinergic Drugs

trihexyphenidyl
Biperiden
Benztropine Mesylate

123
Q

Drugs used for physiological and essential tremor

A

Beta blocker like Propranolol

124
Q

Drugs used for central or physiological tremor

A

Beta 2 blocker

125
Q

Drugs used for Huntington’s disease or Tourette’s?

A

Dopamine blockers (haloperidol or phenothiazine)

126
Q

These drugs work to decrease cholinergic activity in Alzheimer’s. Nausea, bradycardia, myalgia, and tremors are all seen.

4 drugs
Which is not in the US
Which is used as patch
Which is noncompetitive
Which is competitive
Which is hepatotoxic
A

Centrally acting cholinesterase inhibitors

Tacrine: Not in US, Hepatotoxic
Donepezil
Rivastigmine: Patch, noncompetitive
galantamine: Competitive

127
Q

This drug slows the progression of dementia. It works as an NMDA_receptor antagonist in order to decrease glutamine overstimulation of those receptors. Adverse effects mimic dementia.

A

Memantine

128
Q

These drugs work as analgesics for migraines, especially mild ones. (2) One works through vasoconstriction of cerebral arteries.

A

NSAID’s

Caffeine

129
Q

These drugs activate serotonin and sympathetic systems resulting in vasoconstriction of dilated cerebral vessels. Significant first pass effect with metabolites secreted in bile. They are used for acute treatment in migraines. Prolonged use results in rebound headaches. Adverse effects are due to excess vasoconstriction. Contraindicated in CV disease, obesity, hepatic disease, Pregnancy (Category X) and renal disease.

Name the two drugs
Which is in nasal spray form

A

Ergot alkaloids

Ergotamine
Dihydroergotamine: Nasal

130
Q

These drugs inhibit nociceptive transmission and vasoconstrict dilated intracranial extracerebral vessels. They don’t restrict as much as other drugs. Short acting. One is biotransformed by Cyp P450 and others by monoamine oxidase. Vasoconstriction excess causes most side effects. Contraindicated in CV disease, hypertension, MAO inhibitor use, SSRI’s, Ergot use, other durgs in the class.

Name the 6
Which is CYP p450 biotransformed

A

Serotonin-1 Receptor Agonists

Almotriptan
Frovatriptan
Naratriptan: CYP p450 
Rizatriptan
Sumatriptan
Zolmitriptan:
131
Q

These drugs are the drug ofchoice for migraine prevention due to safety. They inhibit vasodilation, renin release, and lipolysis

A

Beta-adrenergic blockers

132
Q

These drugs inhibit cortical depression but have renal, liver, and BM effects.

A

Valproate and other anticonvulsants

133
Q

These drugs inhibit vasculature contraction preceding a migraine. Especially useful in patients who have auras.

A

Calcium channel blockers

134
Q

These drugs are used to prevent migraines. They are inserted into surface vessels of the head. Long duration

A

Botox

135
Q

These should be used for mild migraine

A

Analgesic

136
Q

these should be used for severe migraine (2)
Which has fastest onset
Which is preferred

A

Triptans or ergot alkaloids
Injectable sumatriptan
Triptans are safer

137
Q

Which drug is agent of choice for prevention

A

Beta-adrenergic

Pharmacology (6 decks)

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