Mechanism of Actions Flashcards
What is the MOA of Pyridostigmine?
Prevents the destruction of acetylcholine by acetylcholinesterase allowing nerve impulses to travel across the neuromuscular junction
Although the MOA of ________ is mostly unknown it is thought to inhibit gluatamate release and inactivate voltage-gated Na+ channels in ALS patients.
Riluzole
What Parkinson’s drug’s MOA is listed below……
Restores synaptic concentrations of dopamine
Activates post-synaptic D2 (and some D1) receptors
Levodopa
T/F: Levodopa is not a pro-drug
False
It is the immediate precursor to dopamine
What is the MOA of Carbidopa?
Inhibits dopa-decarboxylase which metabolizes levodopa to dopamine.
This increases the bioavailability levodopa
Are the Ergot Dopamine Receptor Agonists (Bromocriptine, Cabergoline) selective or non-selective D2 receptor agonists?
Selective D2 receptor agonists
Pramipexole has a primary affinity for what dopamine receptor?
D3 (but also D2/4)
T/F: Ropinirole is a D2 receptor agonist
True
Which dopamine receptors does Amorphine act as an agonist at?
D1
D2
What is the MOA of Selegiline and Rasagiline?
Selective and irreversible inhibitors of MAO-B (which metabolizes dopamine)
What class of medication’s MOA is described below……
Inhibit Catechol-O-Methyltranferase which typically metabolizes levodopa top 3-OMD in the brain and periphery
COMT Inhibitors
Talcapone
Entacapone
What Parkinson’s medication’s MOA is described below…..(hint: its an antivrial)
Potentiates dopaminergic function by modifying synthesis, release, or reuptake of dopamine
Amantadine
How do anticholinergics (Trihexyphenidyl, Benzotropine) work in Parkinson’s treatment?
They block the excitatory cholinergic system that presents in dopamine deficiency which helps to alleviate motor dysfunction
What is the MOA of Pimavanserin?
Selective serotonin inverse agonist
High affinity at 5-HT2a
What ALZ medication’s MOA is listed below…..
Reversible inhibition of cholinesterase to prevent acetylcholinesterase hydrolysis
Cholinesterase Inhibitors
Donepezil
Rivastigmine
Galantamine
Which ALZ medication is an uncompetitive NMDA receptor antagonist that works to increase glutamate release in the CNS?
Memantine
The MOA of _________ is mostly unknown, but its immunomodulatory and antiviral effects work to bind to a cell’s surface receptors leading to expression of gene products and markers.
This is used in MS treatment
Interferon Beta
What is the MOA of Mitoxantrone?
Intercalate in DNA causing crosslinks and strand breaks Topoisomerase Inhibitor (like fluoroquinolones) Inhibits T-cells, B-Cells, and Cytokines
Which MS medication’s MOS is described below….
Binds to leukocytes and inhibits adhesion which prevents movement across the BBB
Natalizumab
This MS medication is a Sphingosine 1-phosphate receptor modulator which keeps WBCs in the lymph nodes so they do not cross the BBB
Fingolimod
Which MS medication is a pyrimidine synthesis inhibitor which inhibits immune cells decreasing the number of lymphocytes in the CNS?
Teriflunomide
Dalfampridine is a _____-channel blocker, which _______ (increases/decreases) conduction through demyelinated axons
Potassium-Channel Blocker
Increases Conduction
How does Nudexta (Dextromethorphan/Quinidine) work?
Dexxtro: NMDA receptor antagonist
Quinidine: CYP2D6 Inhibitor, increases bioavailability of dextromethorphan, allowing it to cross the BBB
What class of headache medication’s MOA is listed below…..
Serotonin receptor agonists (5-HT1 receptors)
Mediate vasoconstriction
Triptans
Are ergotamines selective or non-selective 5HT1 receptor agonists?
Do they act as vasodilators or vasoconstrictors?
Non-selective
Vasoconstrictors
Which receptors does DHE bind to?
5HT
NE
DA
Which second line medication for headache treatment is a partial opioid agonist?
Butorphanol
Which pain medication’s MOA is described below…..
Mostly not well understood, but may block cytokines and prostagland release in the CNS
Acetaminophen (Tylenol)
What medication is a glutathione precursor used to metabolize MAPQI?
N-acetylcysteine
What class of pain medications inhibit COX 1 and 2 as well as prostaglandin synthase enzymes
Non-Steroidal Anti-inflammatory Drug (NSAIDs)
T/F: Mistoprostol inhibits gastric acid secretion
True
Which NSAID is a non-selective COX inhibitor, suicide inhibitor, an antiplatelet, and an analgesic?
Aspirin (Acetlysalicylic Acid)
Which class of NSAIDs are semi-selective COX 2 inhibitors?
Enolic Acids
Meloxicam
Prioxicam
Which NSAID is a selective COX 2 inhibitor?
Celecoxib (Celebrex)
What is the general MOA of opioids?
Opioid receptor agonists
Block the release of pain neurotransmitters
Activate pre-synaptic receptors on GABA neurons
Opioids primarily act on which receptor?
What are the subtypes of this receptor?
Mu (Brainstem, Thalamus)
Mu 1: Analgesia, Euphoria
Mu 2: Respiratory Depression, Prolactin Release, Dependence
Other than Mu receptors, what are two additional receptors opioids act on?
Kappa (Analgesia, sedation, respiratory distress)
Delta (Effects not well studied)
Which opioids are full agonists?
Morphine Fentanyl Hydromorphine Codiene Oxycodone Methadone Heroin
Which opioids are partial agonists?
Buprenorphine
Butorphanol
What two medications are opioid antagonists?
Naloxone (Narcan)
Naltrexone
Which two receptors does Oxycodone show activity at?
Mu
Kappa
What receptors does Hydromorphine act on?
Mu
Delta
Which receptor does fentanyl act on?
Mu
T/F: Methadone is also a NMDA antagonist and a SNRI
True
Naloxone is a ____-receptor antagonist used to treat opioid overdose
Mu
Which pain medication’s MOA is described below……
Syntethic codiene analog which inhibits NE and 5HT uptake
Tramadol (Ultram)
What is the MOA of Milnicipran?
Selective serotonin and norepinephrine uptake inhibitor used to treat fibromyalgia
What medication’s MOA is described below…..
Antispasmodic
Potentiates NE
Anticholinergic Activity
Cyclobenzaprine (Flexeril)
What muscle relaxant is a GABA analog which is believed to inhibit relfexes at the spinal cord?
Bacolfen
Other than being an analgesic, Orphenadrine (Norflex) is also an anti-_________.
Anti-Cholinergic
What is the MOA of Glucosamine Sulfate?
Stimulate metabolism of chondrocytes in articular cartilage and synovial cells
Disease modifying effects of OA
What medication is a N-type Ca2+ channel antagonist which blocks excitatory neurotransmitter release?
Ziconotide (Prialt)
What medication’s MOA is described below….
TRPV1 Channel Agonist (inhibits TRPV1 Stimulation)
Depletes substance P
Capsaicin
