Pharm Drug List Test 3

Dopamine Pathways

Nigrostriatal Pathway
VTA/Mesolimbic/Mesocortical
Tuberoinfundibular Neurons
Receptors: D1 family - D1 and D5 (GPCR); D2 family - D2, D3, D4 (GPCR)

Nigrastriatal Pathway

DA Pathway
Function: Posture/Movement
Disorders: Parkinsons Disease

VTA/Mesolimbic/Mesocortical

DA Pathway
Function: target oriented behaviors, addiction, reinforcement
Disorders: Psychoses, drug abuse, depression

Tuberoinfundibular Neurons

DA Pathway
Function: Decreases prolactin secretion from the pituitary
Disorders: hyperprolactinemia

Acetylcholine Pathways

Intrastriatal Neurons
Basal Forebrain Neurons
Mesopontine
Receptors: Muscarinic M1-M5 (GPCR); Nicotinic Neuronal and Non-neuronal (LGIC)

Intrastriatal Neurons

ACh Pathway
Function: Motor activity; activity is inhibited by nigrostriatal neurons
Disorder: Parkinson's Disease

Basal Forebrain Neurons

ACh Pathway
Function: Learning and memory
Disorder: Alzheimer's Disease

Mesopontine Neurons

ACh Pathway
Function: Arousal and REM sleep
Disorder: Narcolepsy?

Serotonin Pathway

Raphe Telencephalic/Diencephalic Projections
Receptors: All are GPCRs except for 5-HT3 which is LGIC

Raphe Telencephalic/Diencephalic Projections

Serotonin pathway
Function: sensory processing and homeostasis
Disorder: Depression/suicide, psychoses, OCD, anxiety

Norepinephrine pathways

Locus Coeruleus - widespread to brain and SC
Lateral Tegmental Nucleus
Receptors: alpha1, alpha2, and beta families (GPCR)

Locus coeruleus projections

NE pathway
Function: learning and memory, attention/arousal
Disorder: depression, narcolepsy

Lateral Tegmental Nucleus

NE pathway
Function: extensive autonomic and neuroendocrine connection/regulation
Disorder: benzodiazepine withdrawl

Histamine Pathway

Lateral tuberomamillary nucleus of hypothalamus projections
Receptors: H1-H4 (GPCR)

Lateral tuberomamillary nucleus projections

Histamine Pathway
Funtion: Arousal, cerebral metabolism, neuroendocrine
Disorder: ???

GABA Pathways

Widespread projections
Receptors: GABAa and GABAc (LGIC), GABAb (GPCR)

Widespread GABA projections

GABA Pathway
Functions: anxiolytic, anticonvulsant, inhibitory actions by causing hyperpolarization
Disorder: anxiety, seizures

Glutamate Pathways

Widespread projections
Receptors: Ionotropic NMDA, AMPA, Kainite (LGIC); Metabotropic mglu1-mglu8 (GPCR)

Widespread Glutamate Projections

Function: synaptic plasticity, learning and memory, pro-convulsant
Disorder: seizures, Alzheimer's disease

l-DOPA

Use: To treat Parkinson's Disease, only decreases the symptoms. Wearing off effect after about 5 yrs of treatment.
Mechanism: Increases DA synthesis in the brain. l-DOPA is a DA precursor and is able to cross the BBB and then get converted to DA. Usually

Carbidopa

Use: Treat PD
Mechanism: Aromatic Amino Acid Decarboxylase (AAAD) inhibitor that doesn't cross the BBB. Prevents peripheral metabolism of l-DOPA to DA by blocking AAAD. Given with l-DOPA to increase the amount of l-DOPA that reaches the brain

Selegiline

Use: Treat early stage of PD and may delay the need for L-dopa or may be used along with L-dopa to enhance the response. Can also be used to treat depression at high doses.
Mechanism: MAO-B inhibitor that blocks the catabolism of DA to DOPAC in the brain.

Amantadine

Use: Treat mild to moderate PD, 6-12 months before initiation of L-dopa.
Mechanism: Antiviral (influenza) that moderately increases DA release, has antimuscarinic activity, and antagonizes NMDA glutamate receptors which possibly protects neurons from glut

Benztropine

Use: Useful in some pts for tremor and drooling; for short term monotherpay in pts with tremor-predominant PD. Little value for akinesia or impaired postural reflexes
Mechanism: Muscarinic receptor antagonist (anticholinergic) that blocks the cholinergic

Bromocriptine

Use: Late in PD once L-dopa no longer works. Not as efficacious as l-DOPA, but lower propensity to cause dyskinesias or motor fluctuations
Mechanism: Ergot derivative that has agonist activity at D1 and D2.
Side Effects:
-Similar side effects as l-DOPA, b

Apomorphine

Use: Given via SC injections. Used for episodes of immobility ("off" times, freezing episodes) in pts with advanced disease
Mechanism: Non-ergot D1 and D2 receptor agonist
Side Effects:
-Similar side effects as l-DOPA, but have more pronounced CNS effects

Donepezil

Use: Symptomatic treatment of Alzheimer's Disease early in the progression. Loses efficacy as disease progresses
Mechanism: AChE inhibitor; used to compensate for loss of ACh in the brain
Side Effects:
-Parasympathetic response due to systemic effects
-N/

Memantine

Use: Symptomatic treatment of AD. Improves ADLs in advanced pts.
Mechanism: Low affinity glutamate NMDA receptor antagonist (amantadine's cousin). May be neuroprotective. Has added effects with ChE inhibitors
Side Effects:
-High doses can produce confusio

Chlorpromazine

Use: Treats positive symptoms of schizophrenia
Mechanism: A typical antipsychotic, phenothiazine. Blocks 70-80% of D2 receptors at clinically effective doses (linear correlation between D2 receptor block and therapeutic potency). Effects come from inhibit

Haloperidol

Use: Treats positive symptoms of schizophrenia
Mechanism: A typical antipsychotic, butyrophenones. Blocks 70-80% of D2 receptors at clinically effective doses (linear correlation between D2 receptor block and therapeutic potency). Effects come from inhibi

Clozapine

Use: Beneficial for positive and negative symptoms of schizophrenia. Atypical antipsychotic
Mechanism: Blocks 40-60% of D2 receptors and 80-90% of 5-HT2A receptors
Side Effects:
-Lower incidence for eps, tardive dyskinesia or hyperprolactinemia than typic

Lithium

Use: First-line/standard treatment for bipolar disorder
Mechanism: May involve alterations in ionic concentrations, neurotransmitter activity, second messenger signaling, GSK-3
-Second messenger signaling: lithium interferes with receptor-activated PI tur

Amitriptyline

Use: Tricyclic Anti-depressant
Mechanism: Non-selectively blocks the reuptake of NE and/or 5-HT to prolong their effects at the nerve terminal. Work via the monoamine hypothesis
Side Effects:
-Anti-autonomic side effects
-Dry mouth
-Weight gain
-Sexual dy

Fluoxetine

Use: SSRI antidepressant
Mechanism: Selectively blocks 5-HT reuptake to prolong their effects at the nerve terminal. Works via the monoamine hypothesis
Side Effects:
-Nervousness, insomnia, and agitations
-Sexual dysfunction

Diazepam aka Valium

Use: Benzodiazepine Anxiolytic. Also has anticonvulsant (status epilepticus), muscle relaxant (depresses spinal reflexes), sedative effects (but decreases REM) preanesthetic. Can be used to treat alcohol withdrawal symptoms
Mechanism: Binding at the benzo

Alprazolam aka Xanax

Use: Benzodiazepine Anxiolytic. Also used as antidepressant, preanesthetic, and to treat acute alcohol withdrawal symptoms
Mechanisms: Binding at the benzodiazepine receptor enhances the ability of GABA to stimulate GABAa receptors and therefore increases

Propranolol

Use: Beta blocker, non-benzodiazepine anxiolytic used for performance anxiety
Mechanism: Suppresses somatic and autonomic symptoms, no effect on emotional symptoms

Zaleplon

Use: Non-benzodiazepine receptor agonist for Insomnia, has no effect on REM
Mechanism: Low abuse potential. May be selective for specific benzodiazepine alpha subunits
Side Effects:
-HA and dizziness
-Back and chest pain
-Migraines
-GI effects
-Nervousnes

Ramelteon

Use: Treats Insomnia
Mechanism: Melatonin Receptor Agonist
Side Effect:
-Somnolence, fatigue, dizziness
-Decreased testosterone and increased prolactin

Phenytoin

Use: Antiseizure drug for partial seizures
Mechanism: Increases Na Channel-mediated inhibition. Prolongs Na Channel inactive state so that it can't be opened even by depolarization. Prevents rapid neuronal firing
Side Effects:
-Side effects are dose-relat

Valproate

Use: Antiseizure
Mechanism: Inhibits T-type Ca Channels, preventing burst of activity required for synchronous activation of cortical neurons. Blocks the thalamocortical loop from initiating abnormal cortical rhythms.
Side Effects:
-Tremor
-N/V
-Elevated

Phenobarbital

Use: Antiseizure Drug
Mechanism: Barbituate. Increase GABA neuronal activity by binding to allosteric site to inhibit surround circuits that normally prevent activation of neurons adjacent to a focus

Baclofen

Use: Antispasmodic agent to treat spasticity
Mechanism: GABA analogue that activates GABA-B receptors on spinal interneurons to promote hyperpolarization. May decrease gamma motor neuron activity and reduce muscle spindle sensitivity

Tizanadine

Use: Antispasmodic agent
Mechanism: Short acting alpha2 agonist that inhibits the release of excitatory amino acids on presynaptic terminals in spinal cord

Dantrolene

Use: Antispasmodic agent that effects skeletal muscles directly
Mechanism: Binds to the ryanodine receptor to inhibit Ca release from SR which uncoulples motor nerve excitation and muscle contraction. Drug of choice for malignant hyperthermia

Acyclovir

Use: Anitviral - herpes simplex virus, Epstein-barr (mono), varicella-zoster virus, cytomegalovirus
Mechanism: Inhibits viral DNA polymerase which inhibits DNA replication.

Zidovudine (AZT-axidothymidine)

Use: Antiviral, HIV, CMV
Mechanism: Reverse transcriptase inhibitor (anti-retroviral). Inhibits HIV reverse transcriptase that converts viral RNA to viral DNA

Cyclophosphamide

Use: Cancer treatment - lymphomas and leukemia, breast and ovarian
Mechanism: Target DNA alkylation and prevents replication
Side Effects: Myelosuppression

Methotrexate

Use: Cancer treatment - leukemia, lymphoma, breast
Mechanism: antimetabolites. Inhibits diydrofolate reductase which leads to decreased DNA and RNA synthesis
Side Effects: Myelosuppression

Imatinib

Use: Cancer treatment
Mechanism: Protein-tyrosine kinase inhibitor that is very selective for cancer cells!
Side Effects: Not as many as other cancer drugs because it targets cancer cells

Penicillin

Use: Antimicrobial, Bacteriocidal for strep, meningitides
Mechanism: Inhibits cell wall synthesis

Cefepime

Use: Antimicrobial - flu, gonorrhoeae
Mechanism: a fourth generation cephalosporin. Inhibits transpeptidase which inhibits cell wall synthesis

Vancomycin

Use: Antimicrobial - MRSA, cdiff, mainly gram positive bacteria
Mechanism: Inhibits cell wall synthesis for mainly gram positive
Side Effects:
-Ototoxicity
-Nephrotoxicity

Gentamicin

Use: Antimicrobial, bacteriocidal - mainly gram negative
Mechanism: Inhibits protein synthesis by binding to the 30s ribosomal subunit and disrupting ribosomal function
Side Effects:
-Ototoxicity
-Nephrotoxicity

Azithromycin

Use: Antimicrobial, bacteriostatic - flu
Mechanism: Inhibits protein synthesis, binds to 50s ribosomal subunit and prevents protein synthesis

Levofloxacin

Use: Antimicrobial - strep, e coli, anthrax, flu
Mechanism: Inhibits DNA gyrase which inhibits DNA replication and leads to cell death
Side Effects: Tendinitis and tendon rupture due to decrease collagen production