Exam 2 Mechanism of Action, Drug Classes & Drugs, Side Effects Flashcards
What does histamine cause?
- vasodilation
- ↑ capillary permeability
- smooth muscle constriction
Antihistamine Mechanism of Action
act as antagonist (block) at H1 receptors
Antihistamine Side Effects
- dizziness
- tinnitus
- incoordination
- blurred vision
- nervousness
- constipation
- weight gain
- insomnia
- tremors
*** paradoxical reaction - drowsiness
First Generation Antihistamine Drugs
- hydroxyzine
- meclizine
- promethazine
What are first generation antihistamines used for?
nausea & vomiting
Second Generation Antihistamine Drugs
- Cetirizine (zyrtec)
- Levocetirizine
- Loratadine (Claritin)
Which antihistamines are sedating & which are non-sedating?
1st Generation = sedating
2nd Generation = non-sedating
Second Generation Antihistamine Mechanism of Action / what is unique about them?
C- cannot cross BBB
- not as effective for N/V
Characteristics of Parkinson’s
- limb rigidity
- tremor
- bradykinesia (slow moving)
- depression, psychosis, anxiety, dementia, etc.
If Parkinson’s disease is caused by too much activity of the GABA neuron due to loss of dopamine, what are the main options for treating Parkinson’s?
vast majority of drugs help the brain make more dopamine or are drugs that act like dopamine. You can also use drugs that block ACh.
What is the main underlying pathophysiological deficit in Parkinson’s Disease?
loss of dopamine releasing neurons in the nitro-striatal pathway
How do drugs that stimulate Dopamine effect the CNS & PNS / what do Dopamine stimulating drugs cause in the CNS & PNS?
CNS: voluntary movement, cognition, motivation, reward/punishment, sleep, inhibition of prolactin
PNS: BP regulation, regulation of peristalsis (inhibition), N/V
Drug Classes used for Parkinson’s Disease
- Dopamine Precursor
- Dopamine Agonists
- Anticholinergic Agents
Drugs for Parkinson’s Disease
- Levodopa (DA precursor)
- Pramipexole (DA agonist)
- Ropinirole (DA agonist)
- Benztropine (Anticholinergic)
Dopamine Precursor Drugs for Parkinson’s Disease
Levodopa
Levodopa Mechanism of Action
neurons can turn Levodopa into dopamine
What is Levodopa given with and why?
Carbidopa to prevent Levodopa from becoming dopamine outside of the brain
Side Effects of Levodopa (Dopamine Precursor)
- Dyskinesia (80%)
- “Wearing Off”
- “On-Off”
- N/V
- Orthostatic Hypotension
- Psychosis
- Sedation
What is “Wearing Off”?
↓ Drug Concentrations = ↑ symptoms
What is “On-Off”?
can happen at any time; not related to concentration
- pt is doing well, then suddenly symptoms come back
Dopamine Agonist Drugs
- Pramipexole
- Ropinerole
Side Effects of Dopamine Agonists
- ↑ hallucinations
- sleepiness
- orthostatic hypotension
- **Impulse Control Disorder **
- N/V
Dopamine Precursor Drugs for Parkinson’s, Mechanism of Action, Contraindications, & Side Effects
Levodopa
MOA: neurons can convert it to dopamine
SE: dyskinesia, “wearing off”, “On-Off”, N/V, orthostatic hypotension, psychosis
Contraindication: do NOT give with food, it’ll slow absorption
Dopamine Agonist Drugs & Side Effects
Pramipexole & Ropinirole
SE: hallucinations, sleepiness, orthostatic hypotension, N/V, syncope, & IMPULSE CONTROL DISORDERS