pharmacology exam 2 drugs

Ambien

a1 subunit binding, works like benzos, minimal muscle relaxing and anticonvulsant effects, amnestic effect, RAPID onset, tolerance with extended use

Zaleplon

a1 subunit binding, works like benzos, tolerance if used over 5-weeks, rapidly absorbed

Eszopiclone

a1 subunit binding, works like benzos, tolerance if used over 6 months

Ramelteon

Melatonin Receptor Agonist

Tasimelteon

Melatonin Receptor Agonist

Suvorexant

orexin receptor antagonist

BuSpar

relieves anxiety without causing marked sedative effects, no withdrawal symptoms, minimal abuse liability

Flumazenil

used to reverse benzodiazepine sedation or to treat benzodiazepine overdose, high affinity competitive antagonist for GABAa receptor and is given IV

Thiobarbituates

very lipid soluble, rapidly enter CNS

Phenobarbital (BENZODIAZEPINE PPT)

low lipid solubility, penetrate brain slowly, affect activity of hepatic drug-metabolizing enzymes and cause increased biotransformation and drug interaction, LONG HALF-LIFE, used for generalized tonic-clonic seizure

Meprobamate

low lipid solubility, penetrate brain slowly, affect activity of hepatic drug-metabolizing enzymes and cause increased biotransformation and drug interaction

Metharbital

used for generalized tonic-clonic seizures

Ureide anti-seizure drug examples

Phenytoin, Primidone, Phenobarbital, Ethosuximide

Phenytoin

voltage-gated sodium channel is the target pre-synoptically to diminish glutamate release, non-sedative but most effective, ADRs include Nystagmus, Diplopia, Ataxia, Purple Glove Syndrome when used as IV

Primidone

metabolized into phenobarbital and PEMA, toxic adverse effects that are similar to phenobarbital

Phenobarbital

chronic treatment of epilepsy because it is less sedative at anti-seizure doses, IV and used to treat drug-refractory status epilepticus, increases the duration of GABAa receptor opening, ADRs include drowsiness, respiratory depression and cardiovascular depression

Ethosuximide

voltage-gated calcium channels is the post-synaptic target at excitatory synapses, inhibits voltage gated sodium channels, ADRs include gastric distress

Tricyclic anti-seizure drug example(s)

Carbamazepine

Carbamazepine

voltage-gated sodium channel is the target pre-synoptically to diminish glutamate release, oral dosage form, increased metabolic capacity of hepatic enzymes, ADRs include diplopia, ataxia, blurred vision and dizziness

Benzos used for anti-seizure/anti-epilepsy

Diazepam, Lorazepam, Clonazepam

Diazepam, Lorazepam

IV or rectally for stopping continuous seizures STATUS EPILEPTICUS

Clonazepam

MOST POTENT ANTISEIZURE DRUG, absence seizures, ADRs include sedation and tolerance

GABA anti-seizure/anti-epilepsy drug examples

Gabapentin, Pregabalin, Vigabatrin

Gabapentin

voltage-gated calcium channel is the target pre-synoptically to diminish glutamate release, approved for treatment of Fibromyalgia, ADRs include somnolence dizziness, ataxia, headache

Pregabalin

blocks Ca2+, generalized tonic-clonic and partial seizures, ADRs include ataxia, dizziness and somnolence

Vigabatrin

increases availability of GABA because it decreases its degradation, irreversible inhibitor of GABA transaminase, used to treat infantile spasms, ADRs include drowsiness, dizziness, weight gain and visual loss

Valproic Acid (Anti-Seizure/Anti-Epilepsy PPT)

blocks sodium channel and increases GABA levels in the brain, human teratogen, INHIBITS METABOLISM OF PHENOBARBITAL AND ETHOSUXIMIDE, valproate displaces phenytoin from plasma proteins

Lacosamide

voltage-gated sodium channel is the target pre-synoptically to diminish glutamate release

Lamotrigine

voltage-gated sodium channel is the target pre-synoptically to diminish glutamate release, it inhibits the opening of those channels and pre-synpatic glutamate release, may interact with Ca channels, FIRST IN LINE TREATMENT, ADRs include dizziness, headache, nausea and SJS

Levetiracetam

binds to synaptic SV2A protein modifies GABA, decreases neuronal glutamate release, ADRs include dizziness, nervousness, depression and seizures

Perampanel

AMPA receptor is the post-synaptic target at excitatory synapses

Retigabine

enhance the natural inhibitory effect of these channels, voltage-gated potassium channel is the target pre-synoptically to diminish glutamate release

Tiagabine

increases availability of GABA, blocks GABA transporter-1, selective inhibitor of GABA tansporter-1, ADRs include dizziness, tremor

Rufinamide

blocks Na channels, Lennox-Gastaut syndrome and focal seizures, ADRs include somnolence, fever, diarrhea

Topiramate

blocks repetitive firing of neurons aka Na channels and potentiates GABA, commonly used for migraine headaches, ADRs include somnolence, fatigue and dizziness

Zonisamide

blocks voltage gated sodium channels, 1 tab PO QD, ADRs include drowsiness, cognitive impairment, renal stones and SJS

Ezogabine

voltage-gated potassium channels is the post-synaptic target at excitatory synapses)

Oxcarbazepine

binds to Na channels and inhibits high-frequency repetitive neuronal firing and inhibits the release of glutamate, less induction of hepatic enzymes

Fosphenytoin

water soluble prodrug

Mephenytoin

metabolized into Nirvanol, ADRs include dermatitis, agranulocytosis, or hepatitis

Ethotoin

not widely used, ADRs include dermatitis, agranulocytosis, or heptatitis

Felbamate

NMDA receptor is the post-synaptic target at excitatory synapses

Dimethadione

voltage-gated calcium channels is the post-synaptic target at excitatory synapses

Trimethadione

blocks T-type calcium channels and raises threshold for seizure discharges, ADRs include sedation

Acetazolamide

diuretic with anti-seizure effects, MOA: mild acidification of the brain, all seizure types, RAPID tolerance

Generalized Tonic-Clonic and Partial Seizures Drugs

Phenyotin, Fosphenyotion, Primidone, Carbamazepine, Gabapentin, Levetiracetam

Partial Seizure Drugs

Pregabalin, Vigabatrin Valproic Acid, Lamotrigine, Topiramate, Tiagabine

Generalized Tonic-Clonic Drugs

Phenyotin, Fosphenyotion, Primidone, Carbamazepine, Gabapentin, Levetiracetam, Tiagabine

Absence Seizure Drugs

Ethosuximide, Clonazepam, Valproic Acid

Myoclonic Seizure Drugs

Clonazepam, Lamotrigine, Valproic Acid, Zonisamide

Levodopa

dopamine does not cross the blood brain barrier, food will delay the appearance of levodopa in the plasma, ADRs include GI, Dyskinesias, Cardiovascular, Behavioral effect

Carbidopa with Levodopa

does not penetrate the BBB

Dopamine Receptor Agonist

Apomorphine, Bromocriptine, Pergolide, Pramipexole, Ropinirole

Ropinirole

D2 agonist, like pramipexole

Bromocriptine

D1, D2 agonist

Pergolide

D1, D2 agonist

ADRs of Dopamine Receptor Agonist

anorexia, vomiting, postural hypotension, arrhythmias, Dyskinesias, confusion and hallucinations

Monoamine Oxidase Inhibitor Drug Examples

Selegiline, Rasgiline

ADRs of MOAIs

Dyskinesia, mental changes, nausea, sleep disorder

COMT inhibitor Drug examples

Tolcapone

Entacapone

Tolpacone

causes hepatoxicity

entacopone

rapid oral absorption

ADRs for COMT inhibitors

Dyskinesias, nausea and confusion

Amantadine

antiviral agent, potentiates dopaminergic function by influencing the synthesis, release, or reuptake of dopamine, agonist of NMDA-type glutamate receptor

Anti-muscarinic ACH blocker drug examples

Benztropine, Trihexyphenidyl, Ethopropazine

Tacrine

non-competitive and irreversible inhibitor of cholinesterase, enters CNS readily after oral administration, SEVERE HEPATIC TOXICITY

Donepezil

reversible inhibitor of acetylcholinesterase, widely prescribed, no hepatotoxicity

Galantamine

reversible, competitive inhibitor of acetylcholinesterase, treats mild to moderate AD)

Rivastigmine

pseudo-irreversible inhibitor of both acetyl and butyryl cholinesterase which means that it initially blocks the enzymes, and it is metabolized by them

true or false: cholinesterase inhibitors penetrate the BBB

true

ADRs for cholinesterase inhibitors

nausea, vomiting and headache

Memantine

glutamate receptor antagonist, moderate to severe Alzheimer's, minor decrease in progression, small but mighty effect on cognition/mood/behavior

ADRs of glutamate receptor antagonist

drowsiness, headache, insomnia and agitation

Lecanemab

for early Alzheimer's, targets amyloid plaques as they form, given 2x/month IV, taken long term

Donanemab

for early Alzheimer's, targets amyloid plaques already formed given 1x/month IV, can be stopped if reached amyloid clearance

Phenothiazine

more affinity to block D2, Alpha1 receptors BUT SOME effect on 5-HT2, M and H1, can be used for anti-itch effects

Aliphatic Phenothiazine

Chlorpromazine

Chlorpromazine

low potency, side effects are due its effect on other receptor inhibition, M block = high sedation, a1 block= hypotensive actions, corneal/lens deposits are the ADRs, more affinity to block D2, Alpha1 receptors BUT SOME effect on 5-HT2, M and H1

Piperidine Phenothiazine

Thioridazine, Mesoridazine

Thioridazine

retinal deposits is ADR, Overdose? Patient will die because ventricular arrhythmias, cardiac conduction block...SUDDEN DEATH. more affinity to block D2, Alpha1 receptors BUT SOME effect on 5-HT2, M and H1

Mesoridazine

Overdose? Patient will die because ventricular arrhythmias, cardiac conduction block...SUDDEN DEATH, more affinity to block D2, Alpha1 receptors BUT SOME effect on 5-HT2, M and H1

Piperazine Phenothiazine

fluphenazine, Trifluoperazine, Prochlorperazine

Fluphenazine

high potency and high extrapyramidal toxicity, INJECTABLE, more affinity to block D2, Alpha1 receptors BUT SOME effect on 5-HT2, M and H1

Prochlorperazine

Antiemetic, more affinity to block D2, Alpha1 receptors BUT SOME effect on 5-HT2, M and H1

Thioxanthenes

more affinity to block D2, Alpha1 receptors BUT SOME effect on 5-HT2, M and H1

Examples of Thioxanthenes

Thiothixene

Thiothixene

high potency, side effects because D2R inhibition, medium extrapyramidal toxicity

Butyrophenone

more affinity to block D2 but some effect on Alpha1

Butyrophenone examples

Haloperidol

Haloperidol

high potency, side effects are because of D2R inhibition, very high extrapyramidal toxicity, can treat Tourette's, INJECTABLE

Clozapine

Blocks D4, Alpha1, 5-HT2, M receptors with a little effect on H1, medium potency, very low extrapyramidal toxicity, last used because can cause seizures and agranulocytosis but given when a patient starts having tardive dyskinesia with other older anti-psychotics

Olanzapine

Blocks 5-HT2 the most, some effect on D2, Alpha 1, M and H1, high potency, low extrapyramidal toxicity

Quetiapine

Blocks 5-HT2 the most, some effect on D2, Alpha 1, M and H1, low potency, low extrapyramidal toxicity

Risperidone

Blocks D2 and 5-HT2 the most, some effect on Alpha 1, M and H1, high potency, low extrapyramidal toxicity

Ziprasidone

Blocks D2, Alpha 1, 5-HT2 with little effect on H1, medium potency, very low extrapyramidal

Aripiprazole

partial agonist at D2 and 5-HT1a, antagonist at 5-HT2A. Block slightly D4, and H1, high potency, very low extrapyramidal

Molindone

Blocks D2 the most, with some effect at Alpha 1, M and H1, can treat Tourette's)

new atypical antipsychotics

clozapine, olanzapine, quetiapine, risperidone, ziprasidone, aripiprazole, molindone, loxapine, pimozide, asenapine, lurasidone

D2 Block

extrapyramidal and endocrine effects, huh??? Relieves hallucinations and improves thought and it slows EEG BUT sleepy and restless. In regard to endocrine, dopamine controls prolactin, messing up dopamine messes up prolactin. In women: galactorrhea, amenorrhea, osteoporosis. In men: gynecomastia, and decreased libido. Also motor defects: early = parkinsonism, late = tardive dyskinesia.