Drug List Flashcards
Memantine
NMDAR
For AD
Low affinity, non-competitive antagonist
Blocks channel in open state (needs to be already activated)
Unbinds very quickly- selectively blocks overactive receptors
Amantadine
NMDAR
PD
Channel blocker, but actually increases channel closure
Likely interacts with multiple receptors (increases DA release), but mechanisms is unknown
Efficacy has been questions, now used in combination therapy
Perampanel
Targets AMPAR- selective non-competitive antagonist (negative allosteric modulator)
For epilepsy
Used in addition to other treatments for partial onset and primary generalized tonic-clonic seizures
Hase serious black box warnings
Black Box Warnings of Perampanel
Psychiatric and behavioural reactions
Aggression, hostility, irritability
Allopregnanolone
Anxiolytic
Approved for postpartum depression
Produced on demand in response to stress
PAM at GABA(A)R
Acute anxiolytic effect
Metabolized by hydroxylation
Synthetic Versions of Allopregnanolone
Aflaxalone
Ganaxolone
Alfaxalone
Anesthetic
Used in veterinary medicine
Ganaxolone
Axiolytic and anticonvulsant
Currently in clinical trials
Atropine
Atropine Sulfate Injection
Non-selective MAChR antagonist
Restores cardiac rate and arterial pressure during anaesthesia when vagal stimulation causes a sudden drop in HR
Lessens degree of AV heart clock when increased vagal tone is a major factor (Too much vagal input damages heart)
Dicyclomine
Dicyclomine Hydrochloride Capsules
Non-Selective mAChR antagonist
Treatment of GI conditions involving smooth muscle spasm (irritable colon i..e IBS) and spastic constipation
Oxybutynin
Oxybutynin chloride extended release tablets
mAChR antagonist
- Selective for M 1,3,4 recepotrs
Relieves symptoms of urgency and frequency of urination in patients with overactive bladder
Decreases contraction of bladder
Nicotine Patch (Nicotine Transdermal System)
Non-selective nAChR agonist
Temporary aid to facilitate smoking cessation
Provides partial substitution for nicotine in cigarettes in order to lessen withdrawal symptoms
Varenicline
Varenicline Tartate tablets
Partial nAChR agonist at alpha4beta2 receptors
Prevent nicotine from binding and inducing DA release from VTA- occupies receptors so that even if you do smoke, it doesn’t have as much as an effect
Smoking cessation treatment in adults in conjunction with smoking cessation counselling
Adverse effects are primarily psychological (suicidal thoughts)
Rivastigmine
Rivastigmine hydrogen tartate
Capsule, oral solution, transdermal patch
Weak AChE inhibitor
Galantamine
Galantamine hydrobromide extended release capsules
Weak AChE inhibitor
Donepezil
Weak AChE inhibitor
Donepezil hydrochloride tablets and rapidly disintegrating tablets
Drugs That Target 5-HT Neurotransmission
Antidepressants
Anti-migraine triptans
Antiemetics
Psychedelic drugs (under investigation for psychiatric disorders)
SSRIs
Fluoxetine
Citalopram
Excitalopram
SNRI
Venlafaxine
Duloxetine
Ergotamine
Anti-migraine triptans
Very promiscuous (5-HT, DA, EPI receptors)
Most preparations removed from market
Available as nasal spray
Sumatriptan/Zolmitriptan
Anti-migraine triptans
Fairy selective for 5-HT1B and 1D
Tablet, subcutaneous injection, nasal spray
Ondansetron
Anti-emetic
Original gold standard
Used as antimetic for chemotherapy and post-surgery
Many products still available in Canada
Palonosetron
Anti-emetic
Newer agent with greater affinity for receptor
For chemotherapy
Methylphenidate
NE and DA reuptake inhibitor (NDRI)
Probably targets DA reuptake more than DA (higher affinity for NE)
One of the first medications for ADHD (Ritalin)
Atomoxetine
NE, DA, 5-HT reuptake inhibitor
Newer medication for ADHD
Affinity NE> 5-HT> DA
Haloperidol
1st generation typical antipsychotics
Antagonist at DA>5-HT receptors
Potential for extrapyramidal adverse effects
Risperidone
2nd generation atypical antipsychotics
Antagonist at DA ~ 5-HT receptors
Less potential for extrapyramidal adverse effects (motor deficits)
Olanzapine
2nd generation atypical antipsychotics
Antagonist at DA ~ 5-HT receptors
Less potential for extrapyramidal adverse effects
Levodopa
Precursor to DA
Majority of dose remains outside of CNS
Conversion to DA induces adverse effects (nausea and vomiting)
Often co-administered with aromatic L-amino acid decarboxylase inhibitor
Benserazie
Aromatic L-amino acid decarboxylase inhibitor
to prevent conversion into DA outside of the brain
Pramipexole
Agonist at D2, D3, D4 receptor
For PD
Adverse effects include nausea and hallucinations
Ropinirole
Agonist at D2, D3, D4 receptor
For PD
Adverse effects include nausea and hallucinations
Loperamide
Agonist at MOR in myenteric plexus
Does not cross BBB (P-glycoprotein transporter will pump it back out)
Decreases activity of longitudinal and circular smooth muscle of intestine
Treats diarrhea
Morphine-
3x stronger than codeine
Fentanyl
50-100x stronger than morphine
Oxycodone
1.5x stronger than morphine
Morphine- Tablet
Morphine Sulfate SR Tablet
Used for pain severe enough to require daily, continuous, long term opioid treatment
Not an “as needed” analgesic
Morphine- Injection
Morphine Sulfact Injection USP
Administered by slow IV injection
Exclusively for symptomatic relief of moderate to severe pain
Not an “as needed” analgesic”
Codeine
Used for mild-moderate pain, often post surgery
Often formulated in combination with an over the counter analgesic
Tylenol with Codeine No. 3
Has acetaminophen, caffeine, codeine phosphate
Lots of black box warnings
Fentanyl- Injection
Fentanyl Citrate Injection
IV or intramuscular injection
For anesthetic or post-operative period (i..e heart surgery, GA)
For C sections
Fentanyl Citrate- Tablets
Buccal/Sublingual
Pain in cancer patients who are tolerant to opioid therapy
Need to work up to dose
Teva-Fentanyl
Transdermal- hard to abuse
only for us in those already receiving opioid therapy
No an “as needed” analgesic
Need to work up to dose
ADHD- Psychostimulants
Amphetamine and methylphenidate
Beneficial for 75% of children affected
Adverse effects Decreased appetite Stomach pain Sleep disturbances Headaches CV disease Potential for dependnece
Methylphenidate
First line of treatment for ADHD
Effective for 75% of patients
Increase DA and NE signalling , taken systemically (can have effects in periphery)
Amphetamine
Blocks reuptake of DA and NE
Induces release of DA
Amphetamine- Dextro/Levo
Enantiomers (mixed salts)
Extended release capsules
Dextroamphetamine
Tablets
Lisdexamfetamine
Pro drug (Amphetamine) For ADHD
Reuptake inhibitor of DA, NE, increases release of DA
Increases amygdala activity
Decreases amygdala-PFC connectivity
Methylphenidate- Intermediate Release
Sustained release
Methylphenidate- Sustained Release
Taken once daily
Extended release tablets
Dose increases throughout day
Methylphenidate- Sustained Release
Taken once daily
Extended release tablets
Dose increases throughout day
Atomoxetine vs Methylphenidate/Amphetamine
Much higher affinity for NE (doens’t boost DA system as much)
NE> 5-HT> DA
Potential therapeutic for those who don’t respond to stimulants, or who cannot tolerate adverse effects
Effects restricted to PFC (low potential for abuse)–> no abuse affinity
Guanfacine
Non-stimulant
Adrenergic α 2 agonist (selective for Alphs2A receptor)
Previously used to lower BP, off label for ADHD
One per day Extended release tablets
Dose titrated up to build tolerance to CV effects
