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185 Cards in this Set

  • Front
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What is the effect of drugs that treat glaucoma?

Decrease intraocular pressure (IOP) via ↓ in amount of aqueous humor (inhibits synthesis / secretion or ↑ drainage)

What are the types of drugs to treat glaucoma?

- α-agonists: Epinephrine and Brimonidine (α2)
- β-blockers: Timolol, Betaxolol, Carteolol
- Diuretics: Acetazolamide
- Cholinomimetics: direct (pilocarpine and carbachol)
- Cholinomimetics: indirect (physostigmine and echothiophate)
- Prostaglandin: Latanoprost (PGF2α)

Drugs to treat glaucoma act how on α receptors? Which drugs?

α-Agonists:
- Epinephrine
- Brimonidine (α2)

What is the mechanism and side effects of using Epinephrine to treat glaucoma?

- Mechanism: ↓ aqueous humor synthesis via vasoconstriction (α-agonist)
- Side effects: Mydriasis (dilation); do not use in closed-angle glaucoma

What is the mechanism and side effects of using Brimonidine to treat glaucoma?

- Mechanism: ↓ aqueous humor synthesis via α2 agonism
- Side effects: blurry vision, ocular hyperemia, foreign body sensation, ocular allergic reactions, ocular pruritus

Drugs to treat glaucoma act how on β receptors? Which drugs?

β-Blockers
- Timolol
- Betaxolol
- Carteolol

What is the mechanism and side effects of using Timolol, Betaxolol, and Carteolol to treat glaucoma?

- Mechanism: ↓ aqueous humor synthesis via β-blockade
- Side effects: no pupillary or vision changes

What diuretic can be used to treat glaucoma?

Acetazolamide

What is the mechanism and side effects of using Acetazolamide to treat glaucoma?

- Mechanism: ↓ aqueous humor synthesis via inhibition of carbonic anhydrase
- Side effects: no pupillary or vision changes

What cholinomimetic drugs can be used to treat glaucoma?

- Direct: Pilocarpine, Carbachol
- Indirect: Physostigmine, Echothiophate

What is the mechanism and side effects of using Pilocarpine and Carbachol to treat glaucoma?

- Mechanism: direct cholinomimetics → ↑ outflow of aqueous humor via contraction of ciliary muscles and opening of trabecular meshwork
- Side effects: miosis and cyclospasm (contraction of ciliary muscle

What is the mechanism and side effects of using Physostigmine and Echothiophate to treat glaucoma?

- Mechanism: direct cholinomimetics → ↑ outflow of aqueous humor via contraction of ciliary muscles and opening of trabecular meshwork
- Side effects: miosis and cyclospasm (contraction of ciliary muscle

Which drug can you use in glaucoma emergencies? Why?

Pilocarpine - very effective at opening meshwork into canal of Schlemm

What prostaglandin drug can be used to treat glaucoma?

Latanoprost (PGF-2α)

What is the mechanism and side effects of using Latanoprost to treat glaucoma?

- Mechanism: prostaglandin (PGF-2α) → ↑ outflow of aqueous humor
- Side effects: darkens color of iris (browning)

What drugs treat glaucoma by decreasing aqueous humor synthesis?

- α-Agonists: Epinephrine and Brimonidine (α2)
- β-Blockers: Timolol, Betaxolol, Carteolol
- Diuretics: Acetazolamide

What drugs treat glaucoma by increasing outflow of aqueous humor?

- Direct Cholinomimetics: Pilocarpine and Carbachol
- Indirect Cholinomimetics: Physostigmine and Echothiophate
- Prostaglandin: Latanoprost (PGF-2α)

What drug has the side effect of darkening the color of the iris (browning)?

Latanoprost (PGF-2α) - prostaglandin used to ↑ outflow of aqueous humor

What are the opioid analgesics?

- Morphine
- Fentanyl
- Codeine
- Loperamide
- Methadone
- Meperidine
- Dextromethorphan
- Diphenoxylate

What is the mechanism of opioid analgesics?

- Act as agonists at opioid receptors to modulate synaptic transmission
- Opens K+ channels, closes Ca2+ channels → ↓ synaptic transmission
- Inhibits release of ACh, NE, 5-HT, glutamate, and substance P

What acts at the µ (mu) opioid receptor?

Morphine

What acts at the δ (delta) opioid receptor?

Enkephalin

What acts at the κ (kappa) opioid receptor?

Dynorphin

How do opioid analgesics modulate synaptic transmission?

- Opens K+ channels
- Closes Ca2+ channels
- ↓ Synaptic transmission

- Inhibits release of ACh, NE, 5-HT, Glutamate, and Substance P

What are the clinical uses of opioid analgesics?

- Pain
- Cough suppression (dextromethorphan)
- Diarrhea (loperamide and diphenoxylate)
- Acute pulmonary edema
- Maintenance programs for heroin addicts (methadone)

What opioid can be used for cough suppression?

Dextromethorphan

What opioid can be used for diarrhea?

- Loperamide
- Diphenoxylate

What opioid can be used in maintenance programs for heroin addicts?

Methadone

What are the possible side effects of opioids?

- Addiction
- Respiratory depression
- Constipation
- Miosis (pinpoint pupils)
- Additive CNS depression with other drugs

What are the characteristics of tolerance to opioids?

Tolerance does not develop to miosis and constipation

How do you treat opioid toxicity?

Naloxone or Naltrexone (opioid receptor antagonist)

What are the partial opioid agonists?

- Butorphanol
- Tramadol

What is the mechanism of Butorphanol?

- Mu-opioid receptor partial agonist
- Kappa-opioid receptor agonist
- Produces analgesia

What is the clinical use of Butorphanol? What is the benefit of this drug over other opioids?

- Severe pain (migraine, labor, etc)
- Causes less respiratory depression than full opioid agonists because it is only a partial mu-opioid agonist

What are the side effects / limitations of Butorphanol?

- Opioid withdrawal symptoms if patient is also taking full opioid agonist (competition for receptors and this drug is only a partial agonist - so acts like antagonist compared to full agonist)
- Overdose not easily reversed with naloxone

What is the mechanism of Tramadol?

- Very week opioid agonist
- Also inhibits serotonin and NE reuptake (works on multiple NTs - "tram it all" in with "tramadol")

What are the clinical uses of Tramadol? Side effects?

- Used for chronic pain
- Side effects: similar to opioids, decreases seizure threshold, serotonin syndrome

Which opioid can cause serotonin syndrome? Why?

Tramadol - it also inhibits serotonin and NE reuptake in addition to its week opioid agonistic activity

What drugs work for simple partial seizures? Which is first line?

** Carbamazepine = First-Line
- Phenytoin
- Valproic acid
- Gabapentin
- Phenobarbital
- Topiramate
- Lamotrigine
- Levetiracetam
- Tiagabine
- Vigabatrin

(Same as for simple partial seizures)

What drugs work for complex partial seizures? Which is first line?

** Carbamazepine = First-Line
- Phenytoin
- Valproic acid
- Gabapentin
- Phenobarbital
- Topiramate
- Lamotrigine
- Levetiracetam
- Tiagabine
- Vigabatrin

(Same as for complex partial seizures)

What drugs work for generalized tonic-clonic seizures? Which is first line?

** Phenytoin = First-Line
** Carbamazepine = First-Line
** Valproic Acid = First-Line
- Gabapentin
- Phenobarbital
- Topiramate
- Lamotrigine
- Levetiracetam

What drugs work for generalized absence seizures? Which is first line?

** Ethosuximide = First-Line
- Valproic acid
- Lamotrigene

What drugs work for status epilepticus seizures?

- Benzodiazepines (diazepam and lorazepam): first line for acute
- Phenytoin: first line for prophylaxis

What drug is first-line for absence seizures? Mechanism?

Ethosuximide
- Blocks thalamic T-type Ca2+ channels

What are the side effects of Ethosuximide?

EFGHIJ:
- "Ethosuximide causes Fatigue, GI distress, Headache, Itching, and stevens-Johnson syndrome"

- Fatigue
- GI problems
- Headache
- Urticaria (itching)
- Steven-Johnson syndrome

What drug is first line for acute status epilepticus? Mechanism?

Benzodiazepines (Diazepam, Lorazepam)
- ↑ GABA-A action

What are the uses and side effects of Benzodiazepines (Diazepam and Lorazepam)?

- Used first line for acute status epilepticus
- Also for eclampsia seizures (1st is MgSO4)
- Side effects: sedation, tolerance, dependence, respiratory depression

What are the uses of Phenytoin? Mechanism?

- First line for tonic-clonic seizures
- First line for prophylaxis of status epilepticus

- ↑ Na+ channel inactivation, zero-order kinetics

What are the side effects of Phenytoin?

- Nystagmus
- Diplopia
- Ataxia
- Sedation
- Gingival hyperplasia
- Hirsutism
- Peripheral neuropathy
- Megaloblastic anemia
- Teratogenesis (fetal hydantoin syndrome)
- SLE-like syndrome
- Induction of cytochrome P-450
- Lymphadenopathy
- Stevens-Johnson syndrome
- Osteopenia

What form of Phenytoin can be taken for parenteral use?

Fosphenytoin

What is Carbamazepine used for? Mechanism?

First-line for:
- Partial simple seizures
- Partial complex seizures
- Tonic-clonic seizures
- Trigeminal neuralgia

Mechanism:
- ↑ Na+ channel inactivation

What are the side effects of Carbamazepine?

- Diplopia
- Ataxia
- Blood dyscrasias (agranulocytosis, aplastic anemia)
- Liver toxicity
- Teratogenesis
- Induction of cytochrome P-450
- SIADH
- Stevens-Johnson syndrome

What drug is first line for trigeminal neuralgia?

Carbamazepine

What is Valproic Acid used for?

- First-line for tonic-clonic seizures
- Also for simple partial, complex partial, myoclonic, and absence seizures
- Also for bipolar disorder

What is the mechanism of Valproic Acid?

- ↑ Na+ channel inactivation
- ↑ GABA concentration by inhibiting GABA transaminase

What are the side effects of Valproic Acid?

- GI distress
- Rare but fatal hepatotoxicity (measure LFTs)
- Neural tube defects in fetus (spina bifida)
- Tremor
- Weight gain
- Contraindicated in pregnancy

What is Gabapentin used for? Mechanism?

Used for:
- Simple partial seizures
- Complex partial seizures
- Tonic-clonic seizures
- Peripheral neuropathy
- Post-herpetic neuralgia
- Migraine prophylaxis
- Bipolar disorder

Mechanism:
- Primarily inhibits high-voltage-activated Ca2+ channels
- Designed as a GABA analog

What are the side effects of Gabapentin?

- Sedation
- Ataxia

What is Phenobarbital used for? Mechanism?

Used for:
- Simple partial seizures
- Complex partial seizures
- Tonic-clonic seizures
- 1st line in neonates

Mechanism:
- ↑ GABA-A action

What are the side effects of Phenobarbital?

- Sedation
- Tolerance
- Dependence
- Induction of cytochrome P-450
- Cardiorespiratory depression

What is Topiramate used for? Mechanism?

Used for:
- Simple partial seizures
- Complex partial seizures
- Tonic-clonic seizures
- Also used for migraine prevention

Mechanism:
- Blocks Na+ channels, ↑ GABA action

What are the side effects of Topiramate?

- Sedation
- Mental dulling
- Kidney stones
- Weight loss

What is Lamotrigine used for? Mechanism?

Used for:
- Simple partial seizures
- Complex partial seizures
- Tonic-clonic seizures
- Absence seizures

Mechanism:
- Blocks voltage-gated Na+ channels

What are the side effects of Lamotrigine?

Stevens-Johnson Syndrome (must be titrated slowly)

What is Levetiracetam used for? Mechanism?

Used for:
- Simple partial seizures
- Complex partial seizures
- Tonic-clonic seizures

Mechanism:
- Unknown, may modulate GABA and glutamate release

What is Tiagabine used for? Mechanism?

Used for:
- Simple partial seizures
- Complex partial seizures

Mechanism:
- ↑ GABA by inhibiting re-uptake

What is Vigabatrin used for? Mechanism?

Used for:
- Simple partial seizures
- Complex partial seizures

Mechanism:
- ↑ GABA by irreversibly inhibiting GABA transaminase

What is Stevens-Johnson Syndrome?

- Prodrome of malaise and fever followed by rapid onset of erythematous / purpuric macules (oral, ocular, genital)
- Skin lesions progress to epidermal necrosis and sloughing

Which epilepsy medications cause Stevens-Johnson Syndrome?

- Ethosuximide
- Phenytoin
- Carbamazepine
- Lamotrigine

Which epilepsy medication causes gingival hyperplasia?

Phenytoin

Which epilepsy medication causes hirsutism?

Phenytoin

Which epilepsy medication causes SLE like syndrome?

Phenytoin

Which epilepsy medication causes blood dyscrasias?

Carbamazepine

Blood dyscrasias:
- Agranulocytosis
- Aplastic anemia

Which epilepsy medication causes neural tube defects?

Valproic acid

Which epilepsy medication causes kidney stones?

Topiramate

Which epilepsy medication causes induction of cytochrome P-450?

- Phenytoin
- Phenobarbital

Which epilepsy medication is used for peripheral neuropathy?

Gabapentin

Which epilepsy medication is used for post-herpetic neuralgia?

Gabapentin

Which epilepsy medication is used for migraine prophylaxis?

- Gabapentin
- Topiramate

Which epilepsy medication is used for bipolar disorder?

- Valproic acid
- Gabapentin

Which epilepsy medication is used first line for neonates?

Phenobarbital

What are the types of barbiturates?

- Phenobarbital
- Pentobarbital
- Thiopental
- Secobarbital

What is the mechanism of barbiturates?

- Facilitate GABA-A actation by ↑ duration of Cl- channel opening
- ↓ Neuron firing → ↑ duration
- Contraindicated in porphyria

In what condition are barbiturates contraindicated?

Porphyria

What are the clinical uses of barbiturates?

- Sedative for anxiety
- Seizures
- Insomnia
- Induction of anesthesia (thiopental)

What are the possible side effects of barbiturates?

- Respiratory and cardiovascular depression (can be fatal)
- CNS depression (can be exacerbated by EtOH use)
- Dependence
- Drug interactions (induces cytochrome P-450)

How do you treat an overdose of barbiturates?

Supportive - assist respiration and maintain BP

What are the types of benzodiazepines?

- Diazepam
- Lorazepam
- Triazolam
- Temazepam
- Oxazepam
- Midazolam
- Chlordiazepoxide
- Alprazolam

What is the mechanism of benzodiazepines?

- Facilitate GABA-A action by ↑ frequency of Cl- channel opening
- ↓ REM sleep

Which benzodiazepines are short-acting? Implications?

Higher addictive potential
- Triazolam
- Oxazepam
- Midazolam

Which benzodiazepines are longer-acting? Implications?

Less addictive potential
- Diazepam
- Lorazepam
- Temazepam
- Chlordiazepoxide
- Alprazolam

What drugs bind the GABA-A receptor?

Ligand-gated Cl- channel:
- Benzodiazepines
- Barbiturates
- EtOH

What are the clinical uses of benzodiazepines?

- Anxiety
- Spasticity
- Status epilepticus (lorazepam and diazepam)
- Detoxification (especially alcohol withdrawal - DTs)
- Night terrors
- Sleep-walking
- General anesthetic (amnesia, muscle relaxation)
- Hypnotic (insomnia)

What are the side effects of benzodiazepines?

- Dependence
- Additive CNS depression effects with alcohol
- Less risk of respiratory depression and coma than with barbiturates

How do you treat an overdose of benzodiazepines?

Flumazenil (competitive antagonist at GABA benzodiazepine receptor)

What are the non-benzodiazepine hypnotics?

All ZZZs put you to sleep:
- Zolpidem (Ambien)
- Zaleplon
- EsZopiclone

What is the mechanism and clinical uses of non-benzodiazepine hypnotics?

- Act via the BZ1 subtype of the GABA receptor
- Used for insomnia

What are the side effects of non-benzodiazepine hypnotics?

- Ataxia
- Headaches
- Confusion
- Short duration because of rapid metabolism by liver enzymes
- Unlike other sedative-hypnotics, cause only modest day-after psychomotor depression and few amnestic effects
- ↓ Dependence risk than benzodiazepines

What are the characteristics of CNS drugs?

CNS drugs must be lipid soluble (cross the blood-brain barrier) or be actively transported

How does the blood and lipid solubility affect anesthetics?

- Drugs with ↓ solubility in blood → rapid induction and recovery times
- Drugs with ↑ solubility in lipids → ↑ potency → 1/MAC

What is the MAC?

Minimal Alveolar Concentration (of inhaled anesthetic) required to prevent 50% of subjects from moving in response to noxious stimulus (eg, skin incision)

What property makes an anesthetic have rapid induction and recovery times?

Drugs with ↓ solubility in blood

What property makes an anesthetic have increased potency?

Drugs with ↑ solubility in lipids

What are the types of inhaled anesthetics?

- Halothane
- Enflurane
- Isoflurane
- Sevoflurane
- Methoxyflurane
- Nitrous oxide

What are the effects of inhaled anesthetics?

- Myocardial depression
- Respiratory depression
- Nausea / emesis
- ↑ Cerebral blood flow (↓ cerebral metabolic demand)

Which inhaled anesthetic causes hepatotoxicity?

Halothane

Which inhaled anesthetic causes nephrotoxicity?

Methoxyflurane

Which inhaled anesthetic causes proconvulsant effects?

Enflurane

Which inhaled anesthetic causes expansion of trapped gas in a body cavity?

Nitrous Oxide

What toxic side effect can all inhaled anesthetics cause?

Malignant hyperthermia - rare, life-threatening hereditary condition in which inhaled anesthetics (except nitrous oxide) and succinylcholine induce fever and severe muscle contractions

How do you treat malignant hyperthermia?

Dantrolene

What are the types of IV anesthetics?

- Barbiturates: Thiopental
- Benzodiazepines: Midazolam
- Arylcyclohexylamines (ketamine)
- Opioids
- Propofol

Which IV anesthetic is high potency and high lipid solubility? Implications?

Barbiturates (Thiopental)
- Rapid entry into brain
- Rapid redistribution

What is Thiopental used for?

- Induction of anesthesia
- Short surgical procedures

What terminates the action of Thiopental?

Terminated by rapid redistribution into tissue (ie, skeletal muscle) and fat

What are the negative effects of Thiopental (IV anesthetic)?

Decreases cerebral blood flow

What is the most common anesthetic used for endoscopy?

Midazolam (benzodiazepine IV anesthetic)

What is Midazolam used for?

- IV anesthetic used for endoscopy
- Adjunctively used with gaseous anesthetics and narcotics

What are the negative effects of Midazolam (IV anesthetic)?

- Post-operative respiratory depression
- ↓ BP
- Anterograde amnesia

What do you give a patient with overdose on IV Midazolam?

Flumazenil

What type of IV anesthetic blocks NMDA receptors?

Arylcyclohexylamines (Ketamine / PCP analog)

What is the mechanism of Ketamine?

- PCP analog
- Dissociative anesthetic
- Blocks NMDA receptors

What are the effects of Ketamine (IV anesthetic)?

- Cardiovascular stimulant
- Hallucinations
- Bad dreams
- ↑ Cerebral blood flow

What types of opioids can be used as IV anesthetics?

- Morphine
- Fentanyl

Use with other CNS depressants during general anesthesia

What anesthetic can be used for sedation in the ICU? Mechanism?

Propofol (IV anesthetic) - potentiates GABA-A

What are the characteristics of Propofol?

- Rapid anesthesia induction
- Good for short procedures
- Less post-op nausea (than thiopental)

What are the types of local anesthetics?

- Esters
- Amides

What are the types of ester local anesthetics?

- Procaine
- Cocaine
- Tetracaine

What are the types of amide local anesthetics?

Amides have 2 I's in name
- Lidocaine
- Mepivicaine
- Bupivacaine

What is the mechanism of local anesthetics?

- Blocks Na+ channels by binding to specific receptors on inner portion of channel
- Preferentially bind to activated Na+ channels, so most effective in rapidly firing neurons

How are tertiary amine local anesthetics different from other local anesthetics?

Penetrate membrane in uncharged form, then bind to ion channels as charged form

How do you enhance the action of local anesthetics?

Give with vasoconstrictors (usually epinephrine) to enhance local action. This decreases bleeding and increases anesthesia by decreasing systemic concentration.

What is the effect of alkaline anesthetics on infected (acidic) tissue?

Alkaline anesthetics are charged and cannot penetrate membrane effectively. Thus, you need more anesthetic.

What is the order of nerve blockade when using local anesthetics?

- small-diameter fibers > large diameter.
- myelinated fibers > unmyelinated
fiers.

Overall, size factor predominates over myelination such that small myelinated fibers > small unmyelinated fibers > large myelinated fibers > large unmyelinated fibers.

What is the order of loss when using local anesthetics?


(1) pain, (2) temperature, (3) touch, (4) pressure.

What are local anesthetics used for?


Minor surgical procedures, spinal anesthesia.

What should you give if patient is allergic to esters?


Give amides.

What are the toxic side effects of local anesthetics?


CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, hypotension, and
arrhythmias (cocaine).

What local anesthetic can cause severe cardiovascular toxicity?


Bupivacaine

What local anesthetic can cause arrhythmias?

Cocaine

What are neuromuscular blocking drugs used for?


Used for muscle paralysis in surgery or mechanical ventilation. Selective for motor (vs. autonomic) nicotinic receptor.

What are the two types of neuromuscular blocking drugs?

Depolarizing and Non-depolarizing

What is an example of a depolarizing blocking drug?


Succinylcholine

What are the effects of Succinylcholine?


Strong ACh receptor agonist; produces sustained depolarization and prevents muscle contraction

What are the phases of blockade?

Phase I (prolonged depolarization)


Phase II (repolarized but blocked; ACh receptors are available, but desensitized)

How do you reverse blockade of depolarizing blocking drugs in Phase I?

Not possible. No antidote. Block potentiated by cholinesterase inhibitors.

How do you reverse blockade of depolarizing neuromuscular blocking drugs in Phase II?


Antidote consists of cholinesterase inhibitors.



What are the complications of depolarizing neuromuscular blocking drugs?


Complications include hypercalcemia, hyperkalemia, and malignant hyperthermia.

What are examples of nondepolarizing neuromuscular blocking drugs?

- Tubocurarine
- Atracurium
- Mivacurium
- Pancuronium
- Vecuronium
- Rocuronium

What is the mechanism of action of nondepolarizing neuromuscular blocking drugs?

Competitive antagonists—compete with ACh for receptors.

What do you give to reverse blockade of nondepolarizing neuromuscular blocking drugs?

- Neostigmine (must be given with atropine to prevent muscarinic effects such as bradycardia)
- Edrophonium, and other cholinesterase inhibitors

What is the mechanism of Dantrolene?


Prevents the release of Ca2+ from the sarcoplasmic reticulum of skeletal muscle.

What are the uses of Dantrolene?


Used to treat malignant hyperthermia and neuroleptic malignant syndrome (a toxicity of antipsychotic drugs).

What syndrome is a toxicity of antipsychotic drugs?

Neuroleptic malignant syndrome

What is Parkinson disease caused by?


Parkinsonism is due to loss of dopaminergic neurons and excess cholinergic activity.

What are the strategies to treat Parkinson disease?

- Use Dopamine Agonists


- Increase Dopamine


- Prevent Dopamine Breakdown


- Curb Excess Cholinergic Activity

What drugs are used as Dopamine agonists in the treatment of Parkinson disease?


- Bromocriptine (ergot)


- Pramipexole


- Ropinirole (non-ergot)



Non-ergots are preferred

What drugs are used to directly stimulate Dopamine in the treatment of Parkinson disease?

- Amantadine (may increase dopamine release)
- L-dopa/carbidopa (converted to dopamine in CNS)

What is a toxicity of Amantadine?

Ataxia

What is Amantadine also used for?

Used as an antiviral against influenza A and rubella.

What drugs are used to prevent Dopamine breakdown in the treatment of Parkinson disease?

- Selegiline (selective MAO type B inhibitor)
- Entacapone, tolcapone (COMT inhibitors - prevent L-dopa degradation which leads to increased dopamine availability)

What drugs are used to curb access cholinergic activity in the treatment of Parkinson disease?

- Benztropine (Antimuscarinic; improves tremor and rigidity but has little effect on bradykinesia)

(Mnemonic: Park your Mercedes-Benz)

What is the mnemonic for drug treatment of Parkinson disease?


BALSA:
- Bromocriptine
- Amantadine
- Levodopa (with carbidopa)
- Selegiline (and COMT inhibitors)
- Antimuscarinics

What drugs do you use for essential or familial tremors?


Use a beta-blocker (e.g., propranolol)

What is the mechanism of L-dopa (levodopa)?

Increases level of dopamine in brain. Unlike dopamine, L-dopa can cross blood-brain barrier and is converted by dopa decarboxylase in the CNS to dopamine.

What is the mechanism of Carbidopa and why is it given with levodopa?

Carbidopa is a peripheral decarboxylase inhibitor, is given with L-dopa to increase the bioavailability of L-dopa in the brain and to limit peripheral
side effects.

What is L-dopa (levodopa) and Carbidopa used for?

Parkinson Disease

What are the toxicities of L-dopa (levodopa) and Carbidopa?

Arrhythmias from increased peripheral formation of catecholamines. Long-term use can lead to dyskinesia following administration (“on-off” phenomenon), akinesia between doses.

What is the mechanism of Selegiline?

Selectively inhibits MAO-B, which preferentially metabolizes dopamine over norepinephrine and
5-HT, thereby increasing the availability of dopamine.



What is Selegiline used for?


Adjunctive agent to L-dopa in treatment of Parkinson disease.

What is the toxicity of Selegiline?


May enhance adverse effects of L-dopa.

What drugs are used to treat Alzheimer?

- Memantine (NDMA receptor antagonist)


- Donepezil, galantamine, rivastigmine (AChE inhibitors)

What is the mechanism of Memantine?


NMDA receptor antagonist; helps prevent excitotoxicity (mediated by Ca2+).

What are the toxicities of Memantine?


Dizziness, confusion, hallucinations.

What is the mechanism of drugs such as Donepezil, galantamine, and rivastigmine?


AChE inhibitors

What are the toxicities of Donepezil, galantamine, and rivastigmine?


Nausea, dizziness, insomnia.

What are the neurotransmitter changes in Huntington disease?

- Decreased GABA
- Decreased ACh
- Increased Dopamine

What are the treatments for Huntington disease?


- Tetrabenazine and reserpine


- Haloperidol

What is the mechanism of Tetrabenazine and Resperine?


Inhibit vesicular monoamine transporter (VMAT); limit dopamine vesicle packaging and release.

What is the mechanism of Haloperidol?


Dopamine receptor antagonist

What is the mechanism of Sumatriptan?


5-HT 1B/1D agonist. Inhibits trigeminal nerve
activation; prevents vasoactive peptide release;
induces vasoconstriction. Half-life < 2 hours.

What are the uses of Sumatriptan?


Acute migraine, cluster headache attacks

What are the toxicities of Sumatriptan?


Coronary vasospasm, mild tingling.

Why is Sumatriptan contraindicated in CAD (Coronary Artery Disease) and Prinzmetal Angina?

Causes Coronary Vasospasm

What is the mnemonic for Sumatriptan?

A SUMo wrestler TRIPs ANd falls on your head.

(SUM + TRIP + AN = SUMATRIPTAN; HEAD = headaches)