Phenytoin (Dilantin)

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Questions and Answers

A patient on phenytoin exhibits nystagmus on lateral gaze, ataxia, and slurred speech. Assuming consistent drug formulation and adherence, which of the following serum phenytoin concentrations is MOST likely contributing to these findings?

  • 45 mg/L
  • 8 mg/L
  • 15 mg/L
  • 25 mg/L (correct)

A patient with a history of tonic-clonic seizures is being initiated on phenytoin. Concurrent medications include an oral contraceptive. To mitigate potential drug interactions, which of the following strategies is MOST appropriate?

  • Recommend a double dose of oral contraceptive to compensate for increased metabolism.
  • Monitor serum phenytoin levels, adjusting the dose based on breakthrough bleeding.
  • Suggest the use of a non-hormonal alternative contraceptive method. (correct)
  • Advise the patient to discontinue the oral contraceptive immediately.

A patient with Alzheimer's disease is currently managed with donepezil. Which mechanism of action BEST describes how this medication aims to alleviate cognitive symptoms?

  • Enhancing glutamate activity at NMDA receptors to improve neuronal signaling.
  • Reversible inhibition of acetylcholinesterase, increasing intrasynaptic acetylcholine. (correct)
  • Increasing beta-amyloid plaque clearance in the brain.
  • Inhibition of acetylcholine synthesis to prevent excitotoxicity.

A patient with mild-to-moderate Alzheimer's disease demonstrates no observable cognitive improvement after several months of donepezil therapy. The physician should first consider?

<p>Evaluating for non-adherence or significant loss of presynaptic acetylcholine release due to disease progression. (B)</p> Signup and view all the answers

A patient with a BMI > 30 presents with both epilepsy and migraine headaches. Which of the following anti-epileptic medications would be MOST appropriate, considering its additional benefit for weight management?

<p>Topiramate (B)</p> Signup and view all the answers

A patient taking topiramate reports a change in taste, specifically noting that carbonated beverages now taste 'flat'. Which explanation MOST accurately describes the underlying mechanism?

<p>Inhibition of carbonic anhydrase, leading to alterations in brain pH that affect sensory perception. (C)</p> Signup and view all the answers

A patient is prescribed duloxetine for depression and anxiety. Given its mechanism of action, what is the MOST LIKELY neurotransmitter effect that contributes to its therapeutic benefit?

<p>Balanced increase in both serotonin and norepinephrine levels in the synaptic cleft. (B)</p> Signup and view all the answers

A patient being treated with venlafaxine for generalized anxiety reports an increase in diastolic blood pressure. What adjustment, if any, is MOST appropriate?

<p>Reduce the dose of venlafaxine and monitor blood pressure closely. (A)</p> Signup and view all the answers

A patient taking fluoxetine reports several adverse effects, including sexual dysfunction and GI upset. The physician is considering adding a medication to mitigate these side effects. Which agent is LEAST likely to exacerbate these issues while maintaining antidepressant efficacy?

<p>Bupropion (B)</p> Signup and view all the answers

A patient with a history of depression is being treated with citalopram. What is the PRIMARY mechanism by which long-term use of citalopram achieves its antidepressant effects?

<p>Downregulation of 5HT receptors and increased neurogenesis. (A)</p> Signup and view all the answers

A patient with epilepsy is being treated with gabapentin. Before initiating therapy, the physician should be aware of which key pharmacokinetic property?

<p>Renal clearance, requiring dosage adjustments in patients with impaired renal function. (C)</p> Signup and view all the answers

A patient presents with confusion, mottling of the extremities, and lower extremity edema while being treated with amantadine. This presentation is highly suggestive of

<p>Livedo reticularis (A)</p> Signup and view all the answers

A patient who abuses opioids is being prescribed gabapentin. What is true regarding gabapentin and opiate abuse?

<p>Gabapentin will not reduce opioid withdrawl. (C)</p> Signup and view all the answers

A patient is prescribed Diazepam (Valium). What receptor does Diazepam bind to?

<p>Located between alpha and gamma subunits of the GABA-A receptor (B)</p> Signup and view all the answers

A child who is not growing while using Ritalin, should do what?

<p>Stop or temporarily stop treatment (B)</p> Signup and view all the answers

A patient who has overdosed on Benzodiazepines is administered Flumazenil (Romazicon). What is the MOA?

<p>Competitive activity at the benzodiazepine receptor site on the GABA/benzodiazepine receptor complex. (A)</p> Signup and view all the answers

If levodopa is used alone, what would occur?

<p>Less than 1% penetrates the CNS (B)</p> Signup and view all the answers

Why is carbidopa/levodopa prescribed?

<p>Carbidopa allows ↑ of dopamine to substantia niagra. (C)</p> Signup and view all the answers

What causes the BB warning of Dantrolene?

<p>Liver damage. (C)</p> Signup and view all the answers

What is one way Memantine causes neuroprotection?

<p>By blocking extra-synaptic NMDA receptors in the CNS (C)</p> Signup and view all the answers

Flashcards

Phenytoin (Dilantin) - MOA

Blocks Na+ channels, increasing GABA-mediated inhibition, decreasing Ca2+ influx to stabilize neuronal membranes without causing general CNS depression.

Phenytoin - Nystagmus

Rhythmic, oscillating eye movement; common early side effect, often requiring dose adjustment.

Donepezil (Aricept) - MOA

Reversibly binds to acetylcholinesterase, increasing acetylcholine levels in the synapse to alleviate cholinergic symptoms of Alzheimer's.

Topiramate (Topamax) - MOA

Blocks voltage-gated Na channels, reduces membrane depolarization and enhances GABA-A receptor activity.

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Common SNRIs - MOA

Inhibit serotonin transporter (SERT) and norepinephrine transporter (NET), enhancing neurotransmission.

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SSRIs - MOA

Blocks serotonin transporter (SERT), leading to enhanced serotonergic neurotransmission; little effect on NET.

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Gabapentin (Neurontin) - MOA & Use

Interact with voltage-gated N-type Ca channels in the CNS, inhibiting excitatory neurotransmitter release; Used to treat seizures, neuropathic pain, migraines

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Amantadine (Symmetrel) - MOA

Alters dopamine (DA) release in the striatum, has anticholinergic properties, and blocks NMDA glutamate receptors.

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Diazepam (Valium) - MOA

Enhance GABA-mediated synaptic inhibition and binds to receptors between alpha and gamma subunits of GABA-A receptor/channel complexes.

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Amphetamines - MOA

Increases the release of norepinephrine, dopamine, and serotonin from nerve terminals.

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Methylphenidate (Ritalin, Concerta) - MOA

Enhances the effects of norepinephrine and dopamine in brain regions to improve attention, concentration, executive function & wakefulness.

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Atomoxetine (Strattera) - MOA

Is a selective norepinephrine reuptake inhibitor that produces therapeutic effects in patients with ADHD.

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Flumazenil (Romazicon) - MOA

Antagonizes the actions of benzodiazepines, binding competitively to benzodiazepine binding sites on GABA-A receptors.

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Carbidopa/Levodopa - MOA

A combo of carbidopa which is an MSD (aromatic amino acid decarboxylase inhibitor), and levodopa, which is a MSD (metabolic precursor of dopamine).

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Dantrolene - MOA

Acts intracellularly in skeletal muscle to lessen the excitation-contraction coupling interaction between actin and myosin within the individual sarcomere

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Memantine (Namenda) - MOA

Blocks extra-synaptic NMDA receptors in the CNS to reduce excessive glutamate-induced excitotoxicity.

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Bupropion (Wellbutrin) - MOA

Inhibit norepinephrine (NE) and dopamine (DA) reuptake by blocking the norepinephrine transporter (NET) and dopamine transporter (DAT).

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Mirabegron (Myrbetriq) - MOA

Causes relaxation of the detrusor muscles during the storage phase of micturition cycle, reducing irritative voiding symptoms or number of incontinence episodes

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Neostigmine (Prostigmin) - MOA

Enhances cholinergic action by facilitating the transmission of impulses across neuromuscular junctions.

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Ambien (Zolpidem) MOA

Acts at the benzodiazepine binding site of the GABA-A receptor producing sedative-hypnotic effects but are chemically distinct from traditional benzos

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Study Notes

Phenytoin (Dilantin)

  • It is a hydantoin
  • Other medications include Fosphenytoin and ethotoin
  • It blocks Na+ channels and increases GABA-mediated inhibition which decreases Ca2+ influx
  • It stabilizes the neuronal membrane by altering Na+ influx during nerve impulse generation
  • It exerts anti-seizure activity without general CNS depression
  • It treats all types of focal and tonic-clonic seizures excluding absence seizures and is used for trigeminal neuralgia
  • Side effects includes nystagmus, diplopia & ataxia, ataxia, gingival hyperplasia, hirsutism, sedation, coarsening of facial features (long-term), abnormalities in Vit D metabolism with OM, and fetal hydantoin syndrome
  • Nystagmus occurs early
  • Diplopia & ataxia are the most common dose-related side effects
  • Toxicity can manifest as excitatory signs
  • Lethal levels of toxicity can result in decerebrate rigidity
  • At plasma concentrations less than 10 mg/L leads to Rare side effects
  • Plasma concentrations of 10-20 mg/L may lead to occasional mild horizontal nystagmus on lateral gaze
  • Plasma concentrations of 20-30 mg/L can cause Nystagmus
  • Plasma concentrations of 30-40 mg/L triggers ataxia, slurred speech, tremor, N/V
  • Plasma concentrations of 40-50 mg/L leads to lethargy, confusion, hyperactivity
  • Plasma concentrations greater than 50 mg/L may cause coma & seizures
  • Monitor bone density and any changes in dentition
  • Monitor Cr (baseline), CBC, folate, LFTs, and serum drug levels periodically
  • Monitor blood pressure, ECG, and respiratory function continuously during and 20 minutes after IV load
  • Get dental exams every 3 months
  • Monitor for depression, behavior changes, and SI ideation
  • Contraindications includes sinus bradycardia, 2nd or 3rd AV block, and sinoatrial block
  • It is important to replace folic acid when taking, as Dilantin blocks absorption
  • Increases metabolism of contraceptives, increasing risk of unplanned pregnancy

Donepezil (Aricept)

  • It is a reversible cholinesterase inhibitor
  • It is an anticholinesterase and a noncovalent reversible inhibitor
  • Reversibly binds the active site of acetylcholinesterase.
  • Increases intra-synaptic levels of acetylcholine, alleviating cholinergic symptoms of Alzheimer’s disease
  • It readily crosses the blood-brain barrier, with a 7-fold higher CNS concentration compared to plasma
  • It treats mild to moderate Alzheimer’s disease
  • It produces a small improvement in cognition and daily activities
  • Lack of response in some patients may result from the loss of presynaptic release of acetylcholine, caused by disease progression
  • Common side effects are GI issues (N/V/D, abd pain, anorexia) and CV issues like bradycardia
  • Cholinergic side effects occur in ~20% of patients at typical doses
  • Aricept patient response to cholinesterase inhibitors is variable
  • 30-50% of patients show no observable benefit, while ~20% show a greater than average response
  • Tacrine, approved in 1993, was limited by hepatotoxicity
  • Donepezil, the primary treatment for mild-to-moderate Alzheimer’s, starts at 5 mg daily, increasing to 10 mg if tolerated
  • A 23-mg sustained-release form benefits moderate-to-severe cases
  • Side effects include nasopharyngitis, diarrhea, nausea, vomiting, and rare rhabdomyolysis
  • Co-treatment with memantine shows no added benefit over high-dose donepezil
  • Rivastigmine is available orally and as a patch, and has similar side effects but a higher fatality rate, possibly linked to transdermal misuse
  • Galantamine, is another AChE inhibitor which has a similar profile to donepezil
  • Cholinesterase inhibitors and memantine cross the blood-brain barrier, slowing cognitive decline temporarily without modifying disease pathology
  • Current research focuses on inflammation, neurodegeneration, cholinergic modulation, and amyloid-tau interactions

Topiramate (Topamax)

  • It is a 2nd generation anti-epileptic
  • Blocks voltage-gated Na channels to control sustained depolarizations during seizures
  • Reduces membrane depolarization by AMPA/Kainate receptors
  • Enhances GABA-A receptor activity to enhance inhibitory effects
  • It weakly inhibits carbonic anhydrase where acidosis in the brain partially protects against seizures by downregulating NMDA receptor activity and antagonizes glutamate receptors
  • It manages and treats epilepsy and migraine.
  • Has approval for chronic weight management for individuals with a BMI above 30
  • Common side effects are somnolence, fatigue, weight loss, and nervousness
  • It may precipitate renal calculi due to inhibition of carbonic anhydrase
  • Cognitive impairment means patients may complain about change in taste of carbonated drinks
  • Monitor creatinine and bicarbonate
  • Off label uses include neuropathic pain, psychotropic drug-induced weight gain, ETOH use disorders, cluster HA prevention, binge eating disorder, bulimia nervosa, and obesity with HTN
  • Treats neuralgiform attacks
  • Can be used as adjunctive therapy in BID, unipolar depression, borderline personality disorder, OCD, PTSD, tourette syndrome, and essential tremor
  • It is a sulfamate-substituted monosaccharide that is FDA-approved
  • For Focal-onset or primary generalized tonic-clonic seizures it is used as:initial monotherapy for patients at least 10 years old or adjunctive therapy ( > 2 YO)
  • Can be used for Lennox Gastaut syndrome which has onset > 2 years old
  • Can be used as Migraine HA prophylaxis in adults

Common SNRIs (Duloxetine, Venlafaxine)

  • It is a Serotonin-Norepinephrine Uptake Inhibitor (SNRI)
  • Inhibits serotonin transporter (SERT) & norepinephrine (NET)
  • Prevents 5HT & NE reuptake, leading to enhanced serotonergic & noradrenergic neurotransmission
  • Affects neurotransmitter ↑ Serotonin (5HT) and ↑ Norepinephrine (NE)
  • Used for Depression, anxiety disorders, and PTSD
  • Common side effects are similar to SSRIs like nausea, constipation, insomnia, HA, and sexual dysfunction
  • For chronic treatment give for sustained effects of depression etc.
  • Duloxetine treats depression and anxiety
  • Treats fibromyalgia, diabetic neuropathy, and stress urinary incontinence off-label
  • Venlafaxine is used as a first-line treatment for generalized anxiety disorder and treats depression
  • Venlafaxine off-label treats hot flashes, pain syndromes, autisms, PMDD, and binge-eating disorder and PTSD
  • Venlafaxine SE includes may cause diastolic HTN (Venlafaxine IR)
  • It is contraindicated in Pregnancy
  • Both medications may require dose adjustments for renal/hepatic impairment
  • It is similar to SSRIs where initial inhibition of SERT induces activation of 5HT1A and 5HT1D autoreceptors
  • These ↓ serotonergic neurotransmission by a negative-feedback mechanism until these serotonergic autoreceptors are desensitized
  • The enhanced 5HT concentration in the synapse can interact with postsynaptic 5HT receptors

SSRIs (Fluoxetine)

  • It is a Selective Serotonin Reuptake Inhibitor
  • Blocks serotonin transporter (SERT) to prevent 5HT reuptake, leading to enhanced serotonergic neurotransmission
  • Long-term effects include downregulating 5HT receptors, decreased SERT expression, and increased neurogenesis
  • It is a first-line treatment for anxiety
  • Treats depression, OCD, and PTSD
  • SERT selective, with little effect on NET
  • Treats PMDD
  • Can treat Perimenopausal and Vasovagal symptoms
  • Common side effects includes sexual dysfunction, GI upset, Serotonin Syndrome (when combined with other serotonergic drugs) and Weight gain
  • It causes a Risk of bleeding, mania/hypomania, seizures, and may increase SI or behavior
  • Causes serotonin syndrome with MAOIs
  • Has numerous drug-drug interactions mediated by CYPs, sexual dysfunction, weight gain (less with vilazodone), and GI disturbances
  • Has Antimuscarinic side effects like dry mouth, urinary retention, and confusion
  • Causes insomnia, increased anxiety, and irritability
  • Decreases libido
  • Causes erectile dysfunction, anorgasmia, and ejaculatory delay (more with paroxetine)
  • Causes nausea, diarrhea, vomiting, dulling of intellectual abilities, decreased concentration, and can lead to gradual withdrawal of medication
  • It is contraindicated in Pregnancy
  • It is used in combination with atypical antipsychotics for treatment resistant MDD
  • Medications used in combination include: ARIPIPRAZOLE (ABILIFY) + SSRI/SNRI, QUETIAPINE (SEROQUEL) + SSRI/SNRI, and OLANZAPINE (ZYPREXA) + FLUOXETINE (PROZAC)
  • Is a first-line treatment for depression due to fewer side effects than TCAs and MAOIs
  • Primary mechanism is serotonin reuptake. It is used to terminate 5HT neurotransmission
  • Long-term use cause leads to receptor desensitization and increases serotonergic tone, explaining delayed antidepressant effects (typically 4-6 weeks)

Gabapentin (Neurontin)

  • It is an Antiepileptic
  • It interacts with voltage-gated N-type Ca channels in the CNS
  • Shows high affinity for binding sites throughout the brain correspondent to the presence of voltage-gated Ca channels, especially alpha-2-delta-1
  • Seems to inhibit the release of excitatory neurotransmitters in the presynaptic area which participate in epileptogenesis
  • Treats seizures, focal seizures, movement disorders, depression/anxiety, ETOH withdrawal, and postherpetic neuralgia
  • Can treat migraines as a preventative
  • Is a first-line treatment for neuropathic pain and peripheral neuropathy
  • Side effects includes GI irritation, weight gain, sedation & dizziness, unsteadiness, and nystagmus
  • Serious Reaction includes suicidality, depression, SJS, anaphylaxis, angioedema, erythema multiforme, rhabdomyolysis, and withdrawal seizure or withdrawal symptoms if discontinued abruptly
  • Monitor creatinine Clearance
  • If creatinine Clearance is less than 60 mL/min then use 1,200 mg/24 hr formulation
  • Medication is cleared renally and excreted unchanged in the urine
  • It doesn't have a high risk of an OD but can increase the euphoria caused by opioids and reduce drug withdrawals
  • Can bypass the blocking effects of addiction treatment medications and does not show up in UDS

Amantadine (Symmetrel)

  • It is an NDMA receptor agonist and a Glutamate antagonist
  • Used as adjunct to levodopa with dose-related fluctuations and dyskinesias
  • Alters dopamine (DA) release in the striatum, has anticholinergic properties, and blocks NMDA glutamate receptors
  • Used in the management of tremor, rigidity, and bradykinesia
  • Used as initial therapy of mild Parkinson’s Disease
  • Causes Dizziness, lethargy, anticholinergic effects, and sleep disturbance and can cause N/V
  • Considerations for elderly is they are prone to confusion.
  • May cause livedo reticularis (diffuse mottling of extremities with LLE)

Diazepam (Valium)

  • It is a Benzodiazepine
  • Enhances GABA-mediated synaptic inhibition and binds to receptors located between alpha and gamma subunits of GABA-A receptor/channel complexes
  • Minimizes seizures and associated neuronal toxicity
  • Used in Status epilepticus (SE) but is NOT 1st line
  • Used as a muscle relaxant
  • Treats anxiety disorders, ETOH withdrawal, skeletal muscle relaxation, can be given as a preanesthetic medication
  • Can treat Meniere disease off-label
  • Side effects includes, hypotonia, dysarthria, and dizziness
  • In children: aggression, hyperactivity, irritability
  • Has a long half-life of 20-80hrs

Adderall, Ritalin and Atomoxetine HCL

  • Amphetamines (Adderall) is an Indirectly acting sympathomimetic
  • Increases the release of norepinephrine, dopamine, and serotonin from nerve terminals
  • Treats Attention-deficit disorders (ADD) and narcolepsy
  • Causes nervousness, insomnia, palpitations, HTN, hyperpyrexia, HA, dizziness, anorexia, weight loss, and dryness of mouth
  • Methylphenidate (Ritalin, Concerta) enhances effects of norepinephrine and dopamine in brain regions that can improve attention, concentration, executive function, and wakefulness
  • Enhancement of dopamine actions in the basal ganglia may improve hyperactivity
  • Enhancement of dopamine & norepinephrine in the medical prefrontal cortex & hypothalamus may improve depression, fatigue & sleepiness
  • treats Attention deficit hyperactivity disorder (ADHD) in children & adults
  • Treats narcolepsy(metadate ER, Methlin ER, Ritalin, Ritalin SR)
  • Is a mild CNS stimulant with more prominent effects on mental than on motor activities
  • May affect BP and should be used with caution in patients in HTN, hyperthyroidism, or history of drug abuse
  • Should avoid in cases of children that are not growing or gaining weight and treatment should STOP (at least temporarily)
  • May inhibit the metabolism of SSRIs so avoid concomitant/overlapping use with MAOIs
  • Stimulants have a high potential of abuse

Atomoxetine (Strattera)

  • It is a Norepinephrine Reuptake Inhibitor and CNS Stimulant
  • Treats ADHD for Children and adults
  • Selective norepinephrine reuptake inhibitor that produces therapeutic effects in patients with ADHD
  • Mechanism of how selective inhibition of presynaptic norepinephrine exerts effects in ADHD has not been determined.
  • One should avoid activities requiring mental alertness or coordination until drug effects are realized
  • Growth rate and weight may need to be monitored more frequently in children
  • Report any new or worsened psychiatric problems, chest pain, palpitation, dyspnea, or s/s of cardiac dysrhythmias, MI, or CVA.
  • Safety and effectiveness not established in children under 6 years of age
  • There is an increased risk of suicidal ideation in short-term studies in children or teens with ADHD
  • Monitor patients closely for suicidality (suicidal thinking and behavior)
  • Hepatic dosing is as follows: Class B initial and target doses should be reduced to 50% of normal dose, Class C initial and target doses should be reduced to 25% of normal dose
  • Renal dosing is not required
  • It cannot be dialyzed
  • Category C in pregnancy so way the risks and benefits
  • Normal metabolizers may have 63% absorption and poor metabolizers may have 94% absorption
  • Food doses do not affect absorption
  • VD is 0.85 L/kg, 98% protein bound
  • Metabolism is extensive and hepatic via CYP2D6 to 1 active metabolite
  • Eliminated renally at 80% and at 17% in feces, with a half-life of 5.2-21.6 hr
  • CYP2D6 poor metabolizers, dose as with drug interaction with CYP2D6 inhibitor
  • Contraindications includes hypersensitivity to atomoxetine, concomitant use of MAOIs, narrow angle glaucoma, adn pheochromocytoma
  • A black Box warning includes pediatric suicidality

Flumazenil (Romazicon)

  • It is a Benzodiazepine receptor antagonist
  • It is a DEA schedule IV drug
  • Antagonizes the actions of benzodiazepines; binds competitively to benzodiazepine binding sites on GABA-A receptors
  • Competitively inhibits the activity at the benzodiazepine receptor site on the GABA/benzodiazepine receptor complex
  • Treats benzo overdose and can be used for reversal of sedative effects during anesthesia
  • Side effects includes dizziness, increased sweating, HA, and abnormal or blurred vision
  • Administration is IV preferred and is given in small injections over 1-3 minutes
  • Contraindications includes patients who have been given a benzo for control of a potentially life-threatening condition (e.g., seizures) and patients showing signs of serious cyclic antidepressant overdose
  • Flumazenil does not antagonize the CNS effect of the drugs affecting GABA-ergic neurons by means other than the benzodiazepine receptor like ethanol, barbiturates, and general anesthesia
  • It can not reverse the effects of opioids
  • Is not effective for other drug overdoses like opioids and barbiturates

Carbidopa/Levodopa (Sinemet)

  • It is a Mainstay treatment for Parkinson’s Disease
  • Composed of a combo of carbidopa, and levodopa
  • Carbidopa is an MSD (aromatic amino acid decarboxylase inhibitor)
  • Levodopa is an MSD (metabolic precursor of dopamine)
  • Treats Parkinson’s Disease
  • Causes Induction of hallucinations and confusion, it happens more in elderly or those with preexisting cognitive dysfunction
  • Drug Interactions: Administration of levodopa with nonspecific inhibitors of MAO accentuates the actions of levodopa and may precipitate life-threatening hypertensive crisis and hyperpyrexia, therefore nonspecific MAO inhibitors should always be discontinued at least 14 days before levodopa is administered
  • Conventional antipsychotics agents, agents are effective against levodopa-induced psychosis but may cause marked worsening of parkinsonism due to actions at the D2 DA receptor and should nt be used in PD. So phenothiazines should be avoided
  • Education is to avoid abrupt withdrawal of levodopa or other dopaminergic medications may precipitate the neuroleptic malignant syndrome of confusion, rigidity, and hyperthermia, a potentially lethal adverse effect
  • If levodopa is used alone, the drug is largely decarboxylated by enzymes in the intestinal mucosa and other peripheral sites so that less than 1% penetrates the CNS
  • Peripheral decarboxylase limits the peripheral decarboxylation to dopamine and increases the bioavailability of levodopa in substantia niagra
  • Initial nausea can be managed by starting carbidopa DAILY
  • The combination reduces the dose of levodopa

Dantrolene

  • acts intracellularly in skeletal muscle to lessen the excitation-contraction coupling interaction between actin and myosin within the individual sarcomere
  • inhibits Ca2+ release from the sarcoplasmic reticulum of skeletal muscle by limiting the capacity of Ca2+ and calmodulin to activate the ryanodine receptor (RYR1)
  • Used in management & prevention of malignant hyperthermia
  • Treats chronic muscle spasticity associated with upper motor neuron disorders (SCI, CVA, CP, or MS)
  • Off-label treats neuroleptic malignant syndrome by blocking the excitation-contraction coupling in the sarcoplasmic reticulum)
  • Can cause skeletal muscle weakness, dyspnea, respiratory muscle weakness, and decreased inspiratory capacity - due to MOA all are expected
  • BB: oral Dantrolene - potential for hepatotoxicity. Therefore Hepatic function should be evaluated before administration and require monitoring throughout the course of treatment. STOP IMMEDIATELY if liver function becomes impaired
  • Peripheral action generalized weakness. Should be reserved for non ambulatory patients with severe spasticity

Memantine (Namenda)

  • It is a NMDA receptor channel antagonist
  • Blocks extra-synaptic NMDA receptors in the CNS
  • Block of NMDA receptor channels may be neuroprotective by reducing excessive (pathologic) glutamate-induced excitotoxicity
  • Treats MOD-SEVERE Alzheimer's disease (AD)
  • Produces a modest effect to reduce the rate of clinical deterioration, no clinical benefit for milder forms of AD
  • Mild side effects includes ha and dizziness
  • Check kidney function
  • Can be used with or without food
  • The medications is Galcanezumab (Emgality), Erenumab (Aimovig), Fremanuzumab (Ajovy), and Atogepant (Qulipta)
  • Is a Class Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist

Peptide (CGRP) Antagonists

  • This class includes Gepants which are monoclonal antibodies and non-peptide small molecules.
  • The monoclonal antibodies are erenumab, eptinezumab, galcanezumab, and fremanezumab
  • This group includes monoclonal antibodies against the CGRP receptor and CGRP receptor antagonists (remegepant and ubogepan);
  • Atogepant and zavegepant are other receptor antagonists that are FDA approved but have no information in PP
  • It prevents and treats acute migraines in adults
  • Common side effects include hypersensitivity (sometimes severe) and injection site reactions
  • Long-term effects: chronic vascular hemodynamic impairment
  • Atogepant (Qulipta) - hightest % of side effects, including serious adverse effects
  • No dosage adjustment for mild-moderate renal impairment; 10 mg daily for patients with severe to end-stage renal disease
  • It is vital to monitor with careful pharmacovigilance and safety monitoring

Ropinirole (Requip)

  • It is a Dopaminergic agonist
  • Can be used in conjunction with lower doses of L-DOPA in a combined therapy approach as monotherapy
  • Targets D2-like receptors and interferes with degradation of dopamine and results in prolonged dopaminergic activity
  • Used to treat Parkinson’s Disease and restless legs syndrome
  • Management of dose-related fluctuation in motor state and may be helpful in preventing motor complications
  • Causes Hallucinosis or confusion, nausea, and orthostatic hypotension, fatigue and somnolence
  • Warn about potential sleepiness, especially while driving

Bupropion (Wellbutrin)

  • is a Norepinephrine-Dopamine Reuptake Inhibitor (NDRI)
  • Inhibits norepinephrine (NE) and dopamine (DA) reuptake by blocking the norepinephrine transporter (NET) and dopamine transporter (DAT)
  • May also increase presynaptic release of NE & DA
  • Effects on the vesicular monoamine transporter (VMAT) may contribute to enhanced neurotransmission
  • It treats Major depressive disorder (MDD) as a monotherapy OR adjunct with SSRIs
  • Also treats seasonal affective disorder (SAD) prevention
  • Has smoking cessation, neuropathy pain, ADHD, and weight loss
  • Results in less sexual dysfunction and less weight gain than SSRIs
  • Common common side effects includes anxiety, tachycardia, HTN, irritability, tremor, HA, nausea, dry mouth, constipation, appetite suppression, insomnia, aggression, impulsivity, agitation
  • Seizures = dose dependent (high risk if greater than 450 mg/day)
  • Renal and hepatic dosing adjustments required
  • Often combined with SSRIs to enhance antidepressant response and counteract SSRI-induced sexual dysfunction and weight gain
  • Contraindicated in patients to avoid if they have seizure disorders lowers SZ threshold
  • Do not give in cases of eating disorders
  • Can not give if there is uncontrolled HTN
  • Drug Interactions: CYP2B6 metabolism; increased risk of seizures with other meds that lower the seizure threshold
  • Activating antidepressant has beneficial for enhancing energy and attention
  • Should not give in cases of seizures or eating disorders
  • Good options to patients concerned about sexual dysfunction or weight gain

Mirabegron (Myrbetriq)

  • It is a B3-Adrenergic Agonist
  • Causes relaxation of the detrusor muscles during the storage phase of micturition cycle, reducing irritative voiding symptoms or number of incontinence episodes
  • 2nd line for overactive bladder/incontinence
  • Requires 4-8 weeks for affects to take hold
  • Side effect includes: HTN, nasopharyngitis, UTI, HA
  • Contraindicated if creatinine clearance is less than 15 mL/min, ESRD, hepatic impairment, and UNCONTROLLED HTN, therefore Monitor: urinary retention and increased BP

Neostigmine (Prostigmin)

  • It is Class Carbamate Anticholinesterase and Cholinomimetic
  • Enhances cholinergic action by facilitating the transmission of impulses across neuromuscular junctions
  • Increases response of myasthenic muscle to repetitive nerve impulses, primarily by the preservation of released endogenous ACh
  • Contains quaternary ammonium group which does not cross the BBB
  • Symptomatic treatment of myasthenia gravis
  • Used off-label, for Non-obstructive ileus which is paralysis of the bowel
  • Side effects include salivation and fasciculation which are visible, involuntary twitching

Ambien (Zolpidem)

  • Novel Benzodiazepine Receptor Agonists/Z compound
  • Alternative treatment for insomnia, sleep disorders and are a safer alternative to barbiturates due to lower abuse potential & better safety profile (agonist to GABA-A) producing sedative effects but are chemically distinct from traditional benozos
  • Little effect on the stages of sleep, does improve sleep latency and prolongs total sleep time
  • May be beneficial for one week following discontinuation with mild rebound insomnia on the first night after d/c
  • More morning sedation (especially if administered late) than Zaleplon
  • daytime drowsiness, cognitive impairment, sleepwalking, and sleep driving in some cases
  • Side effect includes daytime drowsiness, cognitive impairment, sleepwalking, and sleep-driving in some cases
  • Has less potential for dependence compared to benzos but does lead to tolerance and physical dependence with prolonged use
  • Limitations:is less effective than benzodiazepines for conditions like seizures and muscle spasms
  • For short term use
  • Taper gradually to avoid rebound insomnia and other withdrawal symptoms when attempting to withdrawl

Quetiapine (Seroquel)

  • It is an Atypical Antipsychotics
  • has no mechanism of action
  • Has treatment-resistant MDD (combined with antidepressants - SSRIs + SNRIs); OCD - may be less tolerable
  • A side effectis metabolic effects as seen by weight gain, increase lipids
  • Dosings include Acute Antipsychotic for 1st episode and for Chronic treatment.
  • maintenence dose for 1st episode and for chronic treatment.

Buspirone (Buspar)

  • Clas: Non-Benzodiazepine Anxiolytic
  • MOA: partial serotonin and dopamine receptor agonist
  • Treats Generalized Anxiety Disorder (GAD) ONLY (not effective for other anxiety disorders)
  • Does require chronic use and lacks sedative or immediate effects
  • It requires chronic treatment for sustained effects

Lithium

  • Modulates levels of monoamines
  • Alteration of Sodium and Calcium Ion Flow: May alter ion transport by affecting sodium & calcium across membranes so that May alter ion transport by affecting sodium & calcium across membranes. This can change the excitability of neurons so that may alter transport to modulate the flow of dopamine, serotonin, and norepinephrine
  • Inhibition of inositol monophosphatase and modulation of PI pathway therefore Decreased activity of protein kinases, including PKC and GSK-3β for acute prophylaxis,reducing sucidality, neuroprotection and adjunct therapy Effective in reducing suicide
  • Tremors, Cognitive
  • Kidney Effect
  • Narrow TI
  • Slow through Blain Barrier
  • Eliminated after 24 hours
  • Can lead to Toxicity/Overdose
  • Clinical Presentation: Vomiting, diarrhea, tremors, and CNS effects
  • Ebstein anomaly risk
  • Neonatal Effects toxicity
  • Monitor dosing and side effect, suicide risks

Pitolisant (Wakix)

  • It is a H3 Receptor Blockers
  • MOA: Increase histamine activity and are used for narcolepsy treatment and Is an inverse agonist at H3 receptors
  • Signals through 4 GPCR subtypes, influencing adenylyl cyclase or PLC activity
  • Treats Narcolepsy

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