2 disease modifying drugs used to tx MS - MoA - side effects - reduction in relapse rate - administration routes

1. Beta-interferon - MoA - inhibits pro-inflammatory cytokines, T-cell proliferation, CNS trafficking - Side effects - myalgia and chills - Administered - subq and IM - broad impact on inflammation 2. Glatiramer acetate - mixture of amino acids - similar efficacy and side effects as above - give SQ BOTH - 30 to 40% reduction in relapse rate BOTH - tx relapsing remitting and 2ndary progressive MS

Tx for absence epilepsy - include dosing - standard and atypical

Ethosuximide 20 mg/kg/day: Standard Valproic Acid 20 mg/kg/day: If atypical

Major DA systems in the CNS - highest concentration of DA found in which pathway? - which one is the therapeutic target of antipsychotics? - side effects

1. Nigrostriatal - SN to corpus striatum - majority of DA here - SIDE EFFECT -> EPS (movement disorders) 2. Mesolimbic - VTA to nucleus accumbens - THERAPEUTIC SITE 3. Mesocortical - VTA to frontal cortex - THERAPEUTIC SITE 4. Hypothalamus - arcuate nucleus to medial eminence - tuberoinfundibular - prolactin release regulation - SIDE EFFECT -> ENDOCRINE DISORDERS

Neuroleptic Malignant Syndrome - cause - symptoms - treatment

Reaction to antipsychotics (haldol hyperthermia) Symptoms - Hyperthermia - Autonomic Instability - Muscle Rigidity FEVER (from board) - fever - encephalopathy - vitals unstable - elevated enzymes - rigidity of muscles Treatment 1. Withdraw typical antipsychotic 2. Cooling, hydration, supportive care 3. Dantrolene(muscle relaxant) for cooling Bromocriptine (DA receptor agonist)

Exam 6 (drugs only) Flashcards by vase bari

Tx for acute MS relapse

High dose IV methylprednisolone = 1 mg

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2 disease modifying drugs used to tx MS

MoA
side effects
reduction in relapse rate
administration routes

Beta-interferon
- MoA - inhibits pro-inflammatory cytokines, T-cell proliferation, CNS trafficking
- Side effects - myalgia and chills
- Administered - subq and IM
- broad impact on inflammation
Glatiramer acetate
- mixture of amino acids
- similar efficacy and side effects as above
- give SQ

BOTH - 30 to 40% reduction in relapse rate

BOTH - tx relapsing remitting and 2ndary progressive MS

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What 2 drugs are more effective than beta-interferon and glatiramer acetate for txing relapsing remitting and 2ndary progressive MS?

MoA
side effects
administration route

NATALIZUMAB

MoA
- binds to integrin-cellular adhesion molecule
- blocks lymphocytes-endothelial binding which prevents cell from crossing BBB
Administered through IV monthly
Side effects -> PML in 0.2%

FINGOLIMOD

MoA
- blocks egress of lymphocytes from lymph nodes and spleen
Administered orally (unique)
Side effects
- risk of heart block in some w/ initial dose ONLY
- 1 case of PML reported

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2 other oral agents to tx MS

dimethyl fumarate and teriflunomide

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List 2 anticholinergic medications discussed in the dementia lecture

Benztropine (Cogentin)

Trihexyphenidyl (Artane)

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List 2 medications with anticholinergic action

Amitriptyline (Elavil)

Diphenyhydramine (Benadryl)

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Tx for absence epilepsy

include dosing
standard and atypical

Ethosuximide 20 mg/kg/day: Standard

* Valproic Acid 20 mg/kg/day: If atypical

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Major DA systems in the CNS

highest concentration of DA found in which pathway?
which one is the therapeutic target of antipsychotics?
side effects

Nigrostriatal
- SN to corpus striatum
- majority of DA here
- SIDE EFFECT -> EPS (movement disorders)
Mesolimbic
- VTA to nucleus accumbens
- THERAPEUTIC SITE
Mesocortical
- VTA to frontal cortex
- THERAPEUTIC SITE
Hypothalamus
- arcuate nucleus to medial eminence
- tuberoinfundibular
- prolactin release regulation
- SIDE EFFECT -> ENDOCRINE DISORDERS

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Which drug inhibits reuptake in NE neurons but not DA neurons?

Desipramine

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MoA of typical antipsychotics

D2 receptor antagonists

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Extrapyramidal DA side effects of typical antipsychotics

Acute dystonia - Spasm of muscles of face, tongue, neck, and back
Akathisia - Motor restlessness
Parkinsonism - Rigidity, tremor, shuffling gait
Tardive dyskinesia - Oral-facial involuntary movements, choreiform movement of extremities
- late sign

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Neuroleptic Malignant Syndrome

cause
symptoms
treatment

Reaction to antipsychotics (haldol hyperthermia)

Symptoms

Hyperthermia
Autonomic Instability
Muscle Rigidity

FEVER (from board)

fever
encephalopathy
vitals unstable
elevated enzymes
rigidity of muscles

Treatment
1. Withdraw typical antipsychotic
2. Cooling, hydration, supportive care
3. Dantrolene(muscle relaxant) for cooling
Bromocriptine (DA receptor agonist)

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Endocrine DA side effects of typical antipsychotics

-hormonal change and effect

Prolactin INCREASED
Increased lactation, gynecomastia, etc.
Inhibits ovulation, menses
Decreased adrenal corticosteroid secretion
Gonadotropins DECREASED
Inhibits ovulation, menses
Corticotropins DECREASED
Decreased adrenal corticosteroid secretion

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Adverse (non-DA) peripheral effects phenothiazines (e.g., chlorpromazine)

3 groups

Anticholinergic activity
- dry mouth
- blurred vision
- constipation
alpha-adrenoceptor blockade
- orthostatic hypoTN
- inhibition of ejaculation
Endocrine
- appetite increase
- weight gain

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Huntington’s chorea can be txed with?

haloperidol - DA receptor antagonist

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What is a major advantage in using atypical antipsychotics over typicals. Why do we get this advantage?

Much less EPS side effects (D2)

-not completely devoid but have a much higher therapeutic index than typicals

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List 5 atypical antipsychotics (the ones in bold in the ppt)

Aripiprazole
Olanzapine
Clozapine
Quetiapine 
Risperidone

It’s Atypical for Old Closets to Quietly Risper from A to Z

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What’s a disadvantage of atypical antipsychotics? Give examples of this disadvantage

At normal doses, metabolic side effects are significant for atypical drugs

weight gain
metabolic problems
type 2 diabetes

Young and old must be given more attention

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Serious side effect of Clozapine

percent of patients affected
etiology of the side effect?

Agranulocytosis (1-2% of patients; genetic). Testing Essential.

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Which antipsychotic is a partial agonist at D2 DA receptors? Is it typical or atypical

Aripiprazole - atypical

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Compare the efficacy between typical and atypical antipsychotics

Similar efficacy

~70% of patients

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Acamprosate

Reduces the excitatory actions of glutamate at the NMDA receptor

-prevent severe w/drawal from alcohol

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Disulfiram (antabuse)

MoA
side effect

•	Inhibits aldehyde dehydrogenase (ALDH)
•	Use along with psychosocial support 
•	Compliance is an issue
•	Patient needs to monitored
o	Specially if they have other issues (e.g. heart)
•	Not used as much anymore

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Naltrexone

MoA
side effects
check for what before starting?

Study These Flashcards

Good evidence
Anti-relapse drug
Most common side effects = nausea and headache

• Nonselective opiate antagonist
o Reduces the reward component of drinking

• Run a basic liver panel before starting
o Hep B and C

Once a day pill
Use in combination w/ psychosocial treatments for best effect

Acamprosate - MoA - used for

• Modulates the glutamate (indirectly blocks Glu effects on NMDA receptor) • Diminishes post-acute withdrawal o Weeks after people are off substances o This time period is filled with discomfort for the patient • Few side effects

Sustained release Naltrexone - how is it administered? - benefits? - problems?

* Given IM * New and expensive * Addresses compliance * Administered monthly * Vivitrol * Good for people with chaotic lives

Most effective plan to treat alcohol dependence? Least effective?

Naltrexone in combination with medical mngt. found most effective. Behavioral intervention alone, least effective.

List 3 FDA approved pharmacological treatments for quitting nicotine

NRT Bupropion SR Varenicline tartate

NRTs - types - effect on quit rate - precautions

- gum, spray, inhalation - double the quit rate - precautions include 1. pregnancy (class C) 2. CV diseases

Buproprion SR in Treating Nicotine Use Disorder - precaution (2) - contraindications (3) - side effects (2) - effect on quit rate - dosing

-precaution in pregnancy and CV diseases -contraindicated in patients with seizures eating disorders MAOI use w/in the past 14 days -side effects insomnia dry mouth -double quit rate -dosing • Begin 1-2 weeks before quit date • Start at 150mg qAM for 3 days then ↑ to 150mg BID • Maintain this dosage for 7-12 weeks following quit dat

Varenicline tartate - MoA - used for - unique benefit - quit rate

MoA - partial agonist at the alpha4beta2 receptor - causes inhibition of GABA's inhibition of DA - activates release of DA Less cravings and w/drawal side effects Smoking won't lead to the same high -leads to extinction Triples quit rate short term Long term quit rate less

List to off label meds for nicotine use disorder

Nortriptyline and clonidine

Nortriptyline - precautions - side effects - quit rate

-precautions in pregnancy and those w/ CV disease side effects - sedation - dry mouth - urinary retention - risk of OD and cardiotoxicity -doubles the quit rate

Clonidine - precautions - risk of - side effects - quit rate

- preg and CV disease - risk of rebound hypertension (taper dose) - side effects -> dry mouth, drowsiness, sedation and constipation - doubles quit rate

5 C's of addiction

``` Chronic behavioral and mental disorder Control of use impaired Compulsive use Continued use despite harm Craving for the drug ```

Type 1 vs type 2 substance craving behavior - trigger - NTs involved

Type 1 - cue triggered - NT: glutamate Type 2 - stress triggered - CRF in amygdala - NE in brainstem

Major reward site for alcohol

endorphin release by stimulation of mu opiate receptor

How do stimulants (cocaine and amphetamines) work in the brain?

Enhance monoamine NT activity by inhibiting MAO reuptake in synapse o DA – reward o NE – physiological arousal o 5-HT – elevated mood

Mechanism for alcohol w/drawal - 3 things

Decrease in number of GABA receptors Upregulation of NMDA receptors - leads to hyperexcitability - lower seizure threshold Autonomic hyperactivity - inc noradrenergic activity in the LC - Benzos blunt this by stimulating GABA

Opiate w/drawal mech and sxs | -how to reduce the sxs

o Internalization of mu opiate receptors o Increased autonomic activity o Hyperesthesia -Increased perception of pain o Dysphoria o Admin opiate agonists mitigate sxs o Clonidine diminishes noradrenergic effects for LC - Alpha blocker - Reduce the hyperactivity o Nausea, vomiting, diarrhea -Use antiemetic (e.g. Zofran)

Stimulant w/drawal

Deplete DA from reward center (KNOW THIS) • Decreased or lack of substance – Severe dysphoria and drug craving – Sleep disturbances and fatigue

Topomax/topiramate for alcohol w/drawal

Anticonvulsants to regulate manic behavior

Opioid agonists for opiate detox

- methadone - buprenorphine - suboxone

Issue w/ using naltrexone for opiate detox

-must be opiate free for 7 days BLOCK ANALGESIA -lot of pain

Buprenorphine - MoA - why combined with naloxone (suboxone)

Partial mu agonist with HIGH AFFINITY Precipitates w/dawal with recent opiate use - displace opioid from receptor - naloxone added to block action when used IV

Methadone MoA

- full mu agonist - long acting - low misuse potential - tx the w/drawal sxs from opiates

Only activating antidepressant used to tx nicotine w/drawal

Bupropion

Best evidence for NRT use

High dose replacement w/ transdermal + oral breakthrough craving

chantix/varenicline - MoA - black box warning

- partial agonist at nicotinic receptor | - increased suicide risk

Arrange the therapies for depression based on most preferred to least

SSRI > SNRI > Atypicals > TCAs > MAOIs

Side effects of lithium | -decrease in what makes Li+ more toxic?

``` LMNOP Lithium side effects: -Movement (tremor) -Nephrogenic diabetes insipidus -HypOthyroidism -Pregnancy problems ```

Carbamazepine - class - MoA - metabolism - side effects/contraindications

- anticonvulsant - enhances inhibitory action of GABA by inhibiting VG Na channels - induced hepatic (CYP3A4) of itself - lots of drug-drug ix at the level of hepatic metabolism - serious skin rxns in HLA-58 - teratogenic (category D)

Valproic acid - class - MoA - drug-drug ix? - side effects/contraindications

- anticonvulsant - inhibits Na and Ca channels -> activate GABA inhibitory effects - drug-drug interactions due to high serum protein binding - GI complaints; rare hepatic problems, tremor, sedation - Teratogenic (Pregnancy Category D)

SSRIs - there are 4 (use mnemonic) Flashbacks paralyze senior citizens

Fluoxetine, paroxetine, sertraline, citalopram

Side effects of tricyclic antidepressants

Tri-C's: Cardiotoxicity, convulsion, coma

Major side effect of MAOI

hypertensive crisis especially when combined with 6mg tyramine

most common side effects seen with SSRIs?

sexual dysfx and GI probs

Name 2 SNRIs

Venlafaxine, duloxetine

general Rule for naming TCAs

all TCAs end in -iptyline or -ipramine except doxepin and amoxapine imipramine

Exam 6 (drugs only) Flashcards

(59 cards)