How do glaucoma drugs function?
They decrease IOP by decreasing aqueous humor secretion or increasing drainage
Which Glaucoma drugs are alpha receptor agonists?
Epinephrine (alpha-1) and Brimonidine (alpha 2)
List the mechanism of epinephrine in glaucoma
alpha1 agonist; decreases aqueous humor synthesis via vasoconstriction
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!
What is the mechanism of Brominodine
alpha-2 receptor agonist, decreases aqueous humor synthesis
How do beta blockers function in glaucoma?
Decrease aqueous humor synthesis
What are the contraindications/side effects of beta-blockers in glaucoma
None
How does Acetazolamide function in glaucoma?
Diuretic that decreases aqueous humor synthesis via inhibition of carbonic anhydrase
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
What is the use for pilocarpine?
Use in emergencies, very effective at opening meshwork in to Canal of Schlemm
How do physostigmine and echothiophate work in Glaucoma?
Indirect M3 Cholinomimetics, increase outflow of aqueous humor by contracting ciliary muscle and opening trabecular meshwork
Side effects of cholinomimetics in glaucoma?
Miosis and cyclospasm
List the prostaglandin drugs used in glaucoma
Brimatoprost and Latanoprost
How do brimatoprost and latanoprost work?
Increase aqeuous humor outflow, also lead to eyelash growth and darkening of iris
List 8 opioid analgesics
Morphine, fentanyl, codeine, loperamide, methadone, meperidine, dextromethorphan, diphenoxylate, pentazocine
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
What is dextromethorphan used for?
Cough suppression
What are Loperamide and Diphenoxylate used for?
Diarrhea
What are methadone, buprenorphine + nalaxone used for?
Maintenance for heroin addicts
What are opioid analgesics typically used for?
Pain
What are the adverse effects of opioid analgesics?
Addiction, respiratory depression, constipation, miosis (except meperidine), respiratory depression with other drugs
How to treat opioid analgesic toxicity?
Naloxone or Naltrexone
What is the clinical use of pentazocine?
Moderate to severe pain analgesic
What is the mechanism of pentazocine
k-agonist, mu-receptor antagonist
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
- Block presynaptic reuptake of NE and 5HT,
- block cardiac fast Na+ channels,
- antagonize ACh muscarinic receptors,
- antagonize peripheral alpha-1R,
- 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