Pharm Flashcards
(170 cards)
1
Q
What is a cholinergic or cholinomimetic drugs?
A
stimulates the parasympathetic nervous system
2
Q
Pilocarpine
A
Cholin agonist
Treats glaucoma + used to treat xerostomia after radiotherapy
3
Q
Bethenacol
A
Cholin agonist
stims urination
4
Q
Succinylcholine
A
Cholin antagonist
Muscle relaxant for surgery
5
Q
Mecamylamine
A
Cholin antag
Treats hypertension
6
Q
Carbachol
A
Treats closed angle glaucoma
7
Q
Methacholine
A
test reactivity of airway
8
Q
Cevimeline
A
cholin agonist
increase salivary flow
9
Q
Nicotine
A
smoking cessation
10
Q
what are 2 anti-muscarinics ? or anti-muscarinics?
A
atropine
scopolamine
11
Q
what are the effect of anti- muscarinics?
A
dry mouth, blurry vision, urinary retention, constipation
12
Q
what is pralidoxime?
A
a cholinesterase reactivator; use to treat organophosphate poisoning (found in pesticides); relives paralysis of the muscles of respiration.
13
Q
What is glycopyrrolate (Robinul)
A
synthetic anticholinergic
Inhibit salivation pre-operatively; control upper airway secretions
14
Q
What is benztropine mesylate (Cogentin)?
A
synthetic anticholinergic
Anti-Parkinsonism
15
Q
What is Propantheline bromide (Pro-Banthine)?
A
synthetic anticholinergic
Traveler’s diarrhea
16
Q
What is Trihyxphenidyl HCl (Artane)?
A
synthetic anticholinergic
Anti-Parkinsonism
17
Q
List the alpha 1 agonists
A
Epi > NE
phenylephrine
18
Q
List alpha 2 agonists
A
Epi > NE
clonidine
guanfacine
19
Q
List beta 1 agonist
A
Epi = NE
isoprotenerol
dobutamine
20
Q
list beta 2 agonist
A
Epi»_space; NE
isoprotenerol
albuterol
terbutaline
21
Q
What are the tissues that alpha 1 agonists affect?
A
radial muscle of the eye
vasculature
genitourinary/GI sphincters
22
Q
What are the tissues that alpha 2 agonists affect?
A
vasculature
brainstem
NE terminals
23
Q
What are the tissues that beta 1 agonists affect?
A
Heart
24
Q
What are the tissues that beta 2 agonists affect?
A
lungs
vasculature to muscle
ciliary muscle of the eye
genitourinary/uterus
25
what is the antagonist for alpha 1?
prazosin; terazosin
26
what is the antagonist for alpha 2?
yohimbine
27
what is the antagonist for beta 1?
propranolol
atenolol
metoprolol
28
what is the antagonist for beta 2?
propranolol
29
What are the common medications for Parkinson's Disease?
```
L-dopa and carbidopa
Benztropine
Trihexyphenidyl
Selegiline
Entacapone
Azilect
Pramipexole
```
30
What are common drugs that are used in combo with carbidopa-levodopa?
Azilect and Entacapone
31
What is azilect?
Used in conjunction with carbidopa and levodopa (Parkinsons disease) to prevent DA breakdown.
32
What is entacapone?
Used in conjunction with carbidopa and levodopa (Parkinsons disease) to improve carbidopa and levodopa effectiveness
It does this by being an inhibitor of COMT (catechol o methyltransferase); slows down break down of DA
33
What is levodopa?
used to treat parkinson's disease but effectiveness diminishes as disease progresses;
controls the shake, tremors, shuffling
34
What do we combo levodopa with carbidopa?
The problem with levodopa on its own is that it gets metabolized before it gets into the brain by enzymes.
Large doses of L-DOPA = worked but affected other organs, and changed from LDOPA to NE
Resolution was to add Carbidopa to the mix because it is not permeable to the BBB and blocks LDOPA metab occuring outside the blood brain barrier. allowing conversion of LDOPA to DA in the blood brain barrier ie CNS.
35
What are side effects of levodopa and carbidopa?
dyskinesia - abnormal movements
36
If you have a patient that is taking LDOPA and Carbidopa, what should you be concerned with in the dental office?
Be concerned with administering local anesthetics with epinephrine due to the conversion of LDOPA to NE. Synergistic effects of NE and EPI. Avoid epinephrine when possible. But can limit to 3 cartidges of lidocaine 1:100,000 epi per 30 min period to avoid tachycardia and hypertension
37
What is benztropine (cogentin)?
an anticholinergic, to help with sialorrhea since these patients tend to excessively drool
38
what is trehexyphenidyl?
an anticholinergic; to help with sialorrhea since these patients tend to excessively drool
39
what is Pramipexole
D2 agonist
40
what is selegiline?
an MAO (monoamine oxidase inhibitor) used to increase dopaminergic activity
MAO plays an important role in the catabolism of catecholamines (dopamine, norepinephrine and epinephrine) and serotonin.
41
what is pramipexole?
A D2 agonist. Dopamine agonists may be used first to avoid some of the side effects seen with levodopa-carbidopa therapy. Due to breakdown of levodopa into NE during metabolism
42
what are the D1 agonists?
DA
| fendolapam
43
what are the D2 agonists?
DA
| selegiline
44
What tissues do D1 agonists affect?
kidney
vasculature
heart
CNS
45
What tissues do D1 agonists affect on the kidney?
Heart?
Vasculature?
Kidney- increase renal blood volume, GFR, and sodium excretion
Heart/vasculature- vasodilation in renal, cerebral, cardiac, and mesenteric vasculature
46
What tissues do D2 agonists affect?
Post ganglionic sympathetic nerve terminals
Chemoreceptor trigger zone
CNS
47
What tissues do D2 agonists affect on the:
Post ganglionic sympathetic nerve terminals
Chemoreceptor trigger zone
CNS
Post ganglionic sympathetic nerve terminals - decrease NT release
Chemoreceptor trigger zone - nausea/vomitting
48
what is halperidol?
A D2 antagonist
| Treats schizophrenia
49
What should you do if your parkinson's patient is taking selegiline?
do not administer agents with epinephrine because of adverse interactions, causing hypertension
50
What are side effects of L-dopa?
glossodynia (burning tongue), trismus, sialorrhea, dark saliva, dysphagia, bruxism, trismus
51
what are side effects of selegiline?
sublingual oral ulcerations, burning lips, mouth, facial grimacing and supraorbital pain
52
Explain Parkinson's disease
involves degeneration of dopaminergic neurons in the nigral-striatal pathway in the basal ganglia, cause is unknown, but typically associate with hypoxia, toxic chemicals, cerebral infections, and head trauma
Histology: those with parkinson's find lewy bodies
53
What is the strategy behind treating Parkinson's?
1. increase DA in basal ganglia
2. Block muscarinic receptors in the basal ganglia ince cholinergic functions opposes the actions of dopamine in the basal ganglia
54
What system does Huntington's disease affect?
GABA pathways
55
What are the clinical manifestations of huntington's disease?
Abnormal moves (ie corea form) sudden large movements, lack of control with sudden jerky movements.
Cognitive systems begin to deteriorate; progressive intellectual dysfunction
56
What is the pathophysiology of huntington's disease?
Affects GABA and cholinergic striatal cells
| Excessive dopamine activity
57
Medications for huntingtons disease
Antipsychotics (DA antagonists)
Reserpine (DA depletion for choreiform movement)
SSRIs (target seratonin) for depression
Heloperidol (Haldol)- D2 antagonist and antipsychotc
Olanzepine (antipsychotic, binds to DA receptors not just D2)
58
What are the clinical manifestations of early Alzheimer's disease?
short term memory loss; can fake really well, they still value and prioritize information – determines how well they remember that piece of info
Get lost frequently
Still functional
59
What are the clinical manifestations of moderate Alzheimer's disease?
decrease functions, difficulty doing jobs, almost impossible to work ability to cope and be productive is gone at this stage --> stop working
This occurs even in the home
60
What are the clinical manifestations of late Alzheimer's disease?
decrease motor function; no judgement; routine doesn’t work, need assistance from family
Eventually they become immobile and stop eating
Most wil ldie via cachexia
61
What is the pathophysiology of Alzheimer's disease?
```
Beta amyloid (senile palques) form and becomes sticky
Neurofibrillary tangles – clusters of tau protein- it’s a microtuble protein that transports
```
App (amyloid precursor protein)that has been abnormally formed from genetic factors which causes to form sticky Beta amyloid which decrease Ach
62
What type of drugs are used to treat alzheimer's disease?
cholinesterase inhibitors- targets cognitive and functional decline
63
What are examples of cholinesterase inhibitors used for alzheimer's?
donepezil
galantamine
rivastigmine
64
What is multiple sclerosis?
A demyelinating disease, An autoimmune disease that destroys myelin, decreasing action potentials thus becoming less functional.
65
What are the clinical manifestations of MS?
Not all the neurons in the brain are demyelinated but can have multiple sites affected.
Its progressive and relapsing – means a lot of on and off, remission varies in time; with each cycle it gets worse, worse and worse
Diverse effects- dependent on where the damage is located
Autonomics- alters cardio, breathing, GI (super serious)
Senses- hearing, taste, vision
Cognition- ant. Cortex affects how you think and make decisions
Mood- depression, fatigue
66
What medications treat MS?
Steroids to treat inflammation
| ex. Prednisone
67
What is myasthenia gravis?
a chronic autoimmune neuromuscular disease that causes weakness in the skeletal muscles, which are responsible for breathing and moving parts of the body, including the arms and legs.
Myasthenia gravis is caused by an error in the transmission of nerve impulses to muscles. It occurs when normal communication between the nerve and muscle is interrupted at the neuromuscular junction—the place where nerve cells connect with the muscles they control.
In myasthenia gravis, antibodies block, alter, or destroy the receptors for acetylcholine at the neuromuscular junction, which prevents the muscle from contracting.
68
What is the treatment for myasthenia gravis?
Acetylcholinesterase inhibitors such as prostigmine and neostigmine
69
What are anti-psychotic drugs?
1. phenothiazines
2. haloperidol
3. thiothixane
4. atypical antipsychotics
70
What are the 3 derivatives of phenothiazines?
1. aliphatic
2. piperidine
3. piperazine
71
Name the aliphatic derivates of phenothizines
chlorpromaxine
72
Name the piperidine derivates of phenothizines
thioridazine
| mesoridazine
73
Name the piperazine derivates of phenothizines
fluphenazine
perphenazine
prochlorperazine
trifluoperazine
74
which med is resembles piperazine phenothiazines?
halperidol
75
List atypical antipsychotics
```
clozapine
olanzapine
quetiapine
risperidone
ziprasidone
aripiprazole
```
76
What is the mech of action for treatment of psychosis?
Based upon DA hypothesis.
Drugs in the phenothiazine class block DA receptors in the mesolimbic and mesocortical pathways
The key antipsychotic receptor is D2
77
What is mech of action of atypical antipsychotics?
```
Preferentially inhibit selective DA receptors;
Inhibit seratonin (5HT) receptors
```
78
What are adverse effects of antipsychotic drugs?
acute dystonias - sustained muscle contractions
akathisia - a movement disorder characterized by a feeling of inner restlessness and inability to stay still.
parkinsonism - tremor, bradykinesia, rigidity, and postural instability.
perioral tremor
malignant syndrome- idiosyncratic reaction to neuroleptic medications that is characterized by fever, muscular rigidity, altered mental status, and autonomic dysfunction. NMS often occurs shortly after the initiation of neuroleptic treatment, or after dose increases
tardive dyskinesia - stiff, jerky movements of your face and body that you can't control
extrapyramidal effects
antimuscaric effects - adverse motor
orthostatic hypotension
convulsions
photosensitivity
cardiac arrhythmias (long QT)
79
How do antidepressants work?
based on increasing seratonin or NE or both at synapses in selective tracts in the brain; treatment takes several weeks to reach full clinical capacity
80
List antidepressant drugs
1. tricyclic antidepressants
2. SSRIs
3. MAOIs (monoamine oxidase inhibitiors)
4. Misc antidepressants
81
Dopaminergic cells groups and related effects of antipsychotics
1. mesolimbic and mesocortical
2. nigro-striatal
3. tubero-infundibular
4. chemoreceptor trigger zone
5. medullary-periventricular
1. mesolimbic and mesocortical - antipsychotic effects
2. nigro-striatal - motor side effects
3. tubero-infundibular - stim of prolactin release, galactorrhea
4. chemoreceptor trigger zone - antiemetic (effective against vomiting and nausea)
5. medullary-periventricular - increased appetite
82
List of trycyclic antidepressants
```
amytriptyline
desipramine
doxepin
imipramine
protriptyline
```
83
List of SSRIs
```
fluoxetine - prozac
paroxetine - paxil
sertraline - zoloft
fluvoxamine
citalopram - celexa
```
84
List of MAOIs
tranylcypromine
| phenelzine
85
Other antidepressants
```
bupropion
maprotiline
mirtazapine
trazadone
st.johns wort
```
86
What is the action of many antidepressants?
1. Inhibition of reuptake of 5HT, NE, or both
2. increase in synaptic concentrations of NT
3. Desensitization of nerve terminal autoreceptors
4. increase of neuronal release of NTs
5. Selective changes in postsynaptic receptors
87
What is the mechanism of action of tricyclic antidepressants?
inhibit reuptake of 5HT and NE; inhibition of reuptake leads to a sequence of events which eventually result in an antidepressive effect
88
What is the mech of action of SSRIs?
inhibit 5HT
89
what is the mech of action of MAOIs?
inhibit metabolism of NE and 5HT in nerve ending
90
what is the mech of action of St.Johns Worts?
reduces membrane potential of nerves and thus may indirectly reduce uptake of NE and 5HT
91
what is the mech of action of maprotiline
| mirtazapine?
inhibit reuptake of NE and 5HT to varying degrees
92
what is the mech of action of bupropion?
increasing DA in synapses
93
What are the pharmacokinetics of antidepressants?
lipid soluble
long half life
able to be metabolized
94
What are the side effects of tricylic antidepressants?
xerostomia (especially amytriptyline)
hypotension
sedation
antimuscarinic effects***
95
What are the "what not to do's" when administering MAOIs?
to not take it with meds that release 5HT and catecholamines and do not take with other antidepressants
96
What are the side effects of SSRIs?
nausea
vomiting
diarrhea
97
What are the side effects of MAOIs?
hypotension
98
What are the side effects of trazadone?
sedation
| hypotension
99
What are the side effects of bupropion?
very low degree of effects: seizures, hypotension
100
What is the function of dopamine pathways?
- reward (motivation)
- pleasure,euphoria
- motor function
- compulsion
- decision making
101
What is the function of serotonin pathway?
- mood
- memory processing
- sleep
- cognition
102
Why do we use SSRIs to treat depression?
People with depression typically have low serotonin levels thus we want to increase the number or concentration of serotonin in the synapse of nerves.They do this by inhibiting 5ht receptors from re-uptaking 5HT thus accumulation of 5HT begins.
103
What drugs are considered antimania drugs?
lithium
carbamazepine
valproic acid
104
what is the mechanism of action of lithium?
works inside the cell to block conversion of inositol phosphate to inositol; It inhibits excitatory neurotransmitters such as dopamine and glutamate, and promotes GABA-mediated neurotransmission.
105
what is the mechanism of action of carbamazepine?
blocks sodium channels; which prevents repetitive and sustained firing of an action potential
106
what is the mechanism of action of valproic acid
blocks sodium and calcium channels;
attributed to the blockade of voltage-gated sodium channels and increased brain levels of gamma-aminobutyric acid (GABA).
107
What happens chemically is manic (bipolar) patients?
Dopamine neurotransmission is increased. This elevated state would cause downregulation of dopamine receptors. A consequence of downregulation would be decreased dopaminergic neurotransmission associated with clinical depression.
Lithium inducing downregulation of NMDA receptors. As a reminder, the NMDA receptor is a subtype of glutamate receptor. Glutamate is an excitatory neurotransmitter that is elevated during mania.
Lithium increases GABA levels in cerebrospinal fluid. At the presynaptic level, lithium facilitates GABA release. At the postsynaptic level it upregulates GABA-B receptors. (people with manic disorder have low levels of GABA)
108
what are signs of lithium toxicity?
nausea, diarrhea, convulsions, coma, cardiac arrythmias, hypotension,
thyroid enlargement -- increase TSH secretion, may cause hypothyroidism
polydipsia, polyuria
109
What are the clinical applications concerning lithium?
1. patients must be warned against sodium restricted diets because sodium restriction leads to greater retention of lithium by the kidney.
2. lithium inhibits the effect of antidiuretic hormone of the kidney
3. patients must have regular blood checks due to margin of safety is so narrow
110
What are the drug to drug interactions with lithium?
diuretics and newer non-steroidal anti-inflammatory drugs reduce lithium excretion and may cause lithium toxicity
111
what channels are inhibitory?
chloride channels
112
which channels are excitatory?
sodium channels
113
What channels do sedative hypnotics enhance?
chloride channels
114
List sedative hypnotics?
1. benzodiazepines
2. barbituates
3. zolpidem
4. chloral hydrate
5. buspirone
6. baclofen
7. antihistamines
8. ethyl alcohol
115
Benzodiazepines mechanism of action
enhance the effect of GABA at GABAa receptors on chloride channels - increases chloride channel conductance in the brain
116
Barbituates mechanism of action
enhance the effect of GABA on the chloride channel but also increase chloride channel conductance independently of GABA
117
Zolpidem mechanism of action
enhances GABA by BZ1 receptor
118
Choral hydrate mechanism of action
same as barbituates
119
buspirone mechanism of action
partial agonist at a specific serotonin receptor
120
baclofen mechanism of action
stims GABA b receptors -- increase K+ conductance and decrease in Ca2+ conductance
121
antihistamines mechanism of action
block H1 histamine receptors -- leads CNS to sedation
122
what are the pharm effects of benzos?
```
antianxiety
sedation
anticonvulsant
amnesia
relax skeletal muscle
```
123
List 3 benzos
Metabolism?
How fast do these drugs metabolize?
triazolam midazolam alprazolam
rapid route of metabolism via alpha hydroxylations
short sedative actions
124
what are adverse effects of benzos?
```
ataxia (lack of muscle coordination)
confusion
excessive sedation
amnesia
altered sleep patterns
```
125
Long lasting barbituates
List the name of drug?
used for?
phenobarbital
| treats seizures
126
Intermediate lasting barbituates
| used for?
amobarbitol, pentobarbital, secobarbital
| sleep
127
short lasting barbituates
| used for?
hexobarbital, methohexital, thiopental
| rarely used as IV anesthetics
128
```
Benzos:
Dose response profile
therapeutic index
inducer of liver enzyme
respiratory depression
shortens REM sleep
potential for abuse
```
```
Dose response profile- less steep, reaches a plateau at higher doses
therapeutic index- high
inducer of liver enzyme- weak
respiratory depression- lower potential
shortens REM sleep- somewhat
potential for abuse- significant
```
129
```
Barbituates
Dose response profile
therapeutic index
inducer of liver enzyme
respiratory depression
shortens REM sleep
potential for abuse
```
```
Dose response profile- steep no plateau
therapeutic index- low
inducer of liver enzyme- strong
respiratory depression- high potential
shortens REM sleep- to a sig degree
potential for abuse- higher
```
130
Zolpidem
metabolism?
used for?
receptors?
short half lives (about 2 hours)
used for insomnia
selective action at BZ1 receptor -reduces risk of tolerance and dependence
do not have anticonvulsant action
does not greatly affect sleep patterns
131
Chloral hydrate
metabolism?
used for?
receptors?
short acting sleep inducer- metabolized to trichloroethanol
little change on REM sleep
used for conscious sedation in dentistry
132
Buspirone
metabolism?
used for?
abuse potential?
```
short half life (2-4 hours)
relieves anxiety
doesnt act as a anticonvulsant
not a good muscle relaxant
minimum abuse potential
```
133
baclofen
| used for?
used in spasticity to relax skeletal muscle
| occasionally used in trigeminal ganglia
134
example of antihistamines used for sedation
diphenhydramine
135
Sedatives used for muscle relaxation
carisoprodol
cyclobenzaprine
methocarbamol
baclofen
136
What causes seizures?
Inappropriate and excessive activity of motor neurons in the CNS.
137
What are the major receptor targets for antiepileptic drugs?
1. sodium channels
2. receptors assoc with chloride channels
3. T-type calcium channels
4. drugs that inhibit sodium channels, T-type calcium channels, or increase conductance at chloride channels
138
What is the mechanism of phenytoin?
blocks sodium channels
139
What is the mechanism of phenobarbitol?
binds to chloride channel and increases its conductance
140
What is the mechanism of primidone?
binds to chloride channel and increases its conductance
141
What is the mechanism of carbamazepine?
blocks sodium channels
142
What is the mechanism of gabapentin?
increases synthesis and release of gaba
143
What is the mechanism of tiagabine?
binds to chloride channel and increases its conductance
144
What is the mechanism of topiramate?
blocks sodium channels
145
What is the mechanism of lamotrigne?
blocks sodium channels
146
What is the mechanism of vigabatrin?
inhibits GABA reuptake
147
What is the mechanism of valproic acid?
blocks sodium channels and T-type calcium channels
148
What is the mechanism of ethosuximide?
blocks T-type calcium channels
149
What is the mechanism of clonazepam?
binds to chloride channel and increases its conductance
150
What is the mechanism of diazepam?
binds to chloride channel and increases its conductance
151
What is the mechanism of zonisamide?
blocks sodium channels and T-type calcium channels
152
Pharmokinetics of phenytoin
1. slow absorption with oral use
2. antacids may decrease absorption
3. highly bound to plasma protein
4. often zero order elimination kinetics
5. metabolized in liver
153
what are other indications for phenytoin?
trigeminal neuralgia
154
what are the adverse effects of phenytoin?
1. gingival hyperplasia
2. CNS: nystagmus, ataxia, vertigo, diplopia
3. hyperglycemia
4. lymphadenopathy
5. osteomalacia
6. hirsutism
7. deficiency of folate and megaloblastic anemia
8. congenital defects due to utero effects
155
what are other indications for carbamazepine?
1. trigeminal neuralgia
| 2. manic-depressive illness
156
pharmokinetics of carbamazepine
metabolized in the liver; inducer of liver enzymes
157
what are the adverse effects of carbamazepine?
```
GI upset
dizziness, blurred vision
visual disturbances
peripheral neuritis
rashes
jaundice
aplastic anemia and agranulocytosis (rare)
```
158
What are the adverse effects of phenobarbital?
1. sedation
2. neurological and behavioral effects
3. hepatic toxicitiy
4. hypersensitivity leading to hematological effects
5. osteomalacia
6. respiratory depression
159
What are the adverse effects of primidone?
acute systemic and CNS toxicity; sedation, vertigo, nausea, ataxia, diplopia, nystagmus, and hepatic and hematological toxicity
160
what are other indications of gabapentin?
neuropathic pain
161
what are the adverse effects of gabapentin?
sedation
| ataxia
162
what are other indication for valproic acid?
manic depressive illness
163
What are the adverse effects?
```
hair loss
GI upset
hyperglycemia
hyperuricemia
weight gain
hepatic toxicity
thrombocytopenia
teratogenic- may cause spina bifida
```
164
What are the adverse effects of ethosuximide?
GI irritation
CNS depression
Hematological side effects
Lupus
165
what are the drugs of choice for partial seizures?
carbamazepine
phenytoin
topiramate
166
what are the drugs of choice for generalized onset tonic clonic seizures?
valproate, topiramate
167
what are the drugs of choice for absence seizures?
ethosuximide (uncomplicated)
| valproate (complicated)
168
What do general anesthetics do?
reduces pain and consciousness
169
list inhaled anesthetics
halothane
enflurane
isoflurane
sevoflurane
170
list injectable anesthetics
```
propofol
thiopental
droperidol
ketamine
etomidate
```
