Neurobio Pharmacology Flashcards by geet baghel

How do glaucoma drugs function?

They decrease IOP by decreasing aqueous humor secretion or increasing drainage

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Which Glaucoma drugs are alpha receptor agonists?

Epinephrine (alpha-1) and Brimonidine (alpha 2)

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List the mechanism of epinephrine in glaucoma

alpha1 agonist; decreases aqueous humor synthesis via vasoconstriction

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What are the adverse effects of epinephrine in glaucoma?

Mydriasis, blurry vision, ocular hyperemia, allergy reactions, foreign body sensation; DO NOT USE in closed-angle glaucoma!

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What is the mechanism of Brominodine

alpha-2 receptor agonist, decreases aqueous humor synthesis

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How do beta blockers function in glaucoma?

Decrease aqueous humor synthesis

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What are the contraindications/side effects of beta-blockers in glaucoma

None

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How does Acetazolamide function in glaucoma?

Diuretic that decreases aqueous humor synthesis via inhibition of carbonic anhydrase

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Describe the function of Pilocarpine and Carbachol in Glaucoma

Direct M3 Cholinomimetics; increase outflow of aqueous humor via contraction of ciliary muscle and opening of trabecular network

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What is the use for pilocarpine?

Use in emergencies, very effective at opening meshwork in to Canal of Schlemm

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How do physostigmine and echothiophate work in Glaucoma?

Indirect M3 Cholinomimetics, increase outflow of aqueous humor by contracting ciliary muscle and opening trabecular meshwork

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Side effects of cholinomimetics in glaucoma?

Miosis and cyclospasm

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List the prostaglandin drugs used in glaucoma

Brimatoprost and Latanoprost

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How do brimatoprost and latanoprost work?

Increase aqeuous humor outflow, also lead to eyelash growth and darkening of iris

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List 8 opioid analgesics

Morphine, fentanyl, codeine, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate, pentazocine

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How do opioid analgesics function?

Open K+ channels, close Ca+2 channels to decrease synaptic transmission. Inhibit release of ACh, NE, 5HT, glutamate, and substance P

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What is dextromethorphan used for?

Cough suppression

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What are Loperamide and Diphenoxylate used for?

Diarrhea

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What are methadone, buprenorphine + nalaxone used for?

Maintenance for heroin addicts

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What are opioid analgesics typically used for?

Pain

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What are the adverse effects of opioid analgesics?

Addiction, respiratory depression, constipation, miosis (except meperidine), respiratory depression with other drugs

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How to treat opioid analgesic toxicity?

Naloxone or Naltrexone

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What is the clinical use of pentazocine?

Moderate to severe pain analgesic

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What is the mechanism of pentazocine

k-agonist, mu-receptor antagonist

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What is the clinical use of butorphanol?

Severe pain (migraine, labor) analgesic. Causes less respiratory depression than full opioid agonists

What is the mechanism of butorphanol?

k-opioid receptor agonist, mu opioid receptor partial agonist

What is the clinical use of tramadol?

Chronic pain

What are the adverse effects of Tramadol?

Decreases seizure threshold. Serotonin syndrome

What neurotransmitters does tramadol also affect?

Blocks NE and 5HT reuptake

Which drug is the first-line treatment for absence seizures?

Ethosuximide

Describe the mechanism of ethosuximide

Inhibit Thalamic T-Type Ca+2 channels

Describe the side effects of Ethosuximide (EFGHIJ)

Fatigue, GI distress, headaches, itching, Steven-Johnson syndrome

What is the first-line treatment of acute status epilepticus?

Benzodiazepines (Lorazepam, Diazepam, Midazolam)

Describe the function of benzodiazepines

increase GABAa action

List the side effects of benzodiazepines (-pams, and midazolam)

Sedation, tolerance, dependance, respiratory depression

What is the first-line treatment of simple, complex and tonic-clonic seizures in neonates?

Phenobarbital

What is the mechanism of phenobarbital?

increase GABAa action

Side effects of Phenobarbital

Sedation, tolerance, dependence, induction of P450, cardiorespiratory depression

Which two drugs are first-line treatments for grand mal (tonic-clonic) seizures?

Phenytoin and Valproate

What is the mechanism of Phenytoin

Block Na+ channels, zero-order kinetics

Which seizure medication leads to gingival hyperplasia?

Phenytoin

Which seizure drugs induce P450?

Phenobarbital, Phenytoin, Carbamazepine

What are the MSK side effects of phenytoin?

Osteopenia, SLE-like syndrome

What are the hematologic side effects of phenytoin?

Megaloblastic anemia

Which seizure medications are contraindicated in pregnancy?

Phenytoin and Valprate

Which medication if first-line prophylactic against status epilepticus?

Phenytoin

Which drug is first-line for partial simple and complex seizures?

Carbamazepine

How does carbamazepine function?

Blocks Na+ channels

List 7 major side effects of carbamazepine

SIADH!! Ataxia, liver toxicity, aplastic anemia, agranulocytosis, teratogenesis, Steven-Johnson

Which drug is first-line for trigeminal neuralgia?

Carbamazepine

Which drugs are used as migraine prophylaxis?

Valproate and Topiramate

What are 2 mechanisms of Valproate?

Increase Na+ channel inactivation, increase GABA concentration by inhibiting GABA transaminase Block NMDA receptors and affect potassium current

What should be monitored in a patient on Valproate?

LFTs

What other treatments is Valproate used for?

Migraine prophylaxis, Bipolar disorder, myoclonic seizures

Which condition contraindicates use of barbiturates?

Porphyria

Describe the function of barbiturates (phenobarbital, pentobarbital, thiopental, secobarbital)

Increases duration of Cl- channel to facilitate GABAa action

What are barbiturates used for?

Sedative agents, used for anxiety, seizures, insomnia, induction of anesthesia

Side effects of barbiturates

Risky CV depression, CNS depression (worsened by alcohol use), drug interactions (P450)

How to treat barbiturate overdose

Supportive

What is mechanism of Benzodiazepines?

Facilitate GABAa action by increasing frequency of Cl- channel opening

What are the addictive benzodiazepine?

ATOM: Alprazolam, Triazolam, Oxazepam, Midazolam

What are benzodiazepines used for?

Anxiety, status epilepticus, eclampsia, detox from alcohol withdrawal, night terrors, general anesthetic, hypnotic

How to treat benzo overdose?

Flumazenil

What is a complication of Benzodiazepines?

Can precipitate seizures

What are the nonbenzodiazepine hypnotics?

Zolpidem, Zaleplon, esZopiclone

What are the benefits of Zolpidem vs benzos?

Lowered risk of dependence, milder day-after psychomotor depression and few amnestic effects

Mechanism of nonbenzo hypnotics

BZ1 subtype of GABA receptor. Sleep cycle less affected. Side effects include headache, ataxia, confusion. Short duration bc fast liver metabolism

What predisposes someone to Malignant hyperthermia?

AD mutation of voltage-sensitive ryanodine receptor

Trigger and treatment of Malignant hyperthermia

Trigger: Inhaled anesthetics Treatment: Dantrolene (ryanodine receptor antagonist)

What is thiopental used for

Induction of anesthesia

What is midazolam used for

Endoscopy

Order of nerve blockade of local anesthetics

small myelinated -> small unmyelinated -> large myelinated -> large unmyelinated

Order of sensory loss of local anesthetic

Pain, temperature, touch, pressure

How is carbidopa more potent than levodopa?

Inhibits peripheral conversion of L-dopa making it more available to the brain

Which central side effects are associated with levodopa and carbidopa?

Anxiety and agitation

How can tachyarrhythmias be reduced as a side effect when prescribing levo/carbidopa?

Peripheral decarboxylase inhibitor

Which drug leads to aplastic anemia, SIADH, liver toxicity, thrombocytopenia?

Carbamazepine

Which 3 drugs block NMDA receptors in hippocampus?

Ketamine, Felbamate, Memantine

What is Ketamine used for

General anesthesia

What is felbamate used for

anticonvulsant

What is memantine used for

Treatment of Alzheimer dementia

What should be monitored in a patient on carbamazepine?

CBCs

What type of medication is amitryptiline?

Tricyclic antidepressant

What are tricyclic antidepressants used for?

Insomnia, adjunctive pain medications

5 ways TCAs function

1. Block presynaptic reuptake of NE and 5HT, 2. block cardiac fast Na+ channels, 3. antagonize ACh muscarinic receptors, 4. antagonize peripheral alpha-1R, 5. antagonize H1 receptors

Side effects of TCAs

Tremor, hypotension (arrhythmias), confusion, constipation, urinary retention, orthostatic hypotension, sedation

What is gabapentin used for?

Diabetic neuropathy

Which receptors does botulinim toxin inhibit?

Muscarinic (dry mouth, mydriasis, no pupil reflex) and nicotinic (muscle weakness)

Which receptors do TCAs inhibit?

Muscarinic (impaired autonomic symptoms)

What is Topiramate used for

Anticonvulsant to treat epilepsy in children and adults

How does capsaicin inhibit pain?

causes excessive activation of TRPV1, buildup of intracellular calcium that results in dysfunction of nociceptive nerve fibers. Causes release and depletion of substance P

How is postherpatic (shingles) pain typically managed?

with TCAs (amitryptiline) or anticonvulsants (gabapentin, pregabalin)

First-line therapy for depression

SSRIs

Symptoms of serotonin syndrome

hyperreflexia, clonus, rigidity, tremor, agitation, confusion, hyperthermia, tachycardia, vomiting/diarrhea, sweating

Treatment for serotonin syndrome

Cyproheptadine (antihistamine with anti-serotonergic properties)

What is the initial treatment for status epilepticus?

Benzodiazepine (lorazepam) + Phenytoin

Which agents are the best to administer to decrease morbidity/mortality in cerebral vasospasm following SAH?

Calcium channel blockers

What is the most common cause of bacterial meningitis in adults of all ages

Strep pneumo

Which chromosome is amyloid precursor protein located on?

Chromosome 21

How does liquefactive necrosis occur in the brain?

Ischemic neurons release lipids and lysosomes. Microglia migrate into the area and remove the necrotic tissue leaving a cavity. Astrocytes surround cavity to form scar (gliosis)

VDRL positive CSF is indicative of

Neurosyphilis and tabes dorsalis

Propanolol is first-line treatment for

Familial essential tremor

Which drug is most commonly used to treat positive symptoms of psychosis (hallucinations, delusions)

Haloperidol

How do organophosphates leads to excess ACh accumulation

Irreversible achetylcholinesterase inhibitors

Treatment for organophosphate poisoning

Muscarinic antagonists (atropine) and pralidoxamine (binds organophosphates and decouples from AChE)

Restless leg syndrome can be treated with

Dopamine agonists (pramiprexole, ropinirole)

Restless leg syndrome is related to deficiency of which mineral in the substantia nigra?

Iron

Partial opioid agonist that can precipitate opioid withdrawal symptoms in patients with increased opioid tolerance

Buprenorphine

Reduces Parkinson's symptoms by inhibiting COMT and thus Levodopa breakdown in periphery

Entacapone

Prevents Levodopa breakdown in brain by inhibiting COMT

Tolcapone

Halothane, Enflurane, Isoflurane and Sevoflurane

Halogen inhaled anesthetics

Adverse effect of Halogenated anesthetics

Hepatitis (centrilobular hepatic necrosis)

Which antiepileptic is preferred in patients with combined absence and tonic-clonic seizures?

Valproate

Best treatment for restless leg syndrome

Dopamine agonsit (ropinirole or pramiprexole)

First-line treatment for psychomotor agitation associated with alcohol withdrawal

Benzodiazepines

How does long-term use of first and second generation antipsychotics cause tardive dyskinesia

Prolonged D2 blockade leads to upregulation of dopamine receptors in substantia nigra