-
The _____________ test is used to test whether potential
drugs are likely to cause cancer.
Ames
-
Human trials of a new drug on small numbers of sick humans to determine how well it works and to look for adverse effects are phase ____
trials.
Phase I
-
A drug which increases the risk of birth defects is called a
_____________________.
Teratogen
-
This drug caused a flipper like birth defect
Thalidomide
-
It causes p_________________________, the medical name for a
condition in which
babies are born with ____________________________. This drug was being widely
used in __________________, but had not been approved in the
US. More recently this
drug has found use in the treatment of the skin
disease:____________________.
phocomelia,flipper like hands, Germany, acne
-
Accutane is an example of a drug which has a high risk of
causing birth defects and is rated ______.
X
-
______________ is a common OTC drug which can
cause closure of the ductus arteriosus in the fetus.
Ibuprofen
-
A drug such as _________________ which is regarded as completely
safe for pregnant women is rated A on the risk schedule.
Levothyroxine
-
Phase 2 drug metabolism covalently adds a molecule with multiple OH groups called______ onto drug molecules.
glucoronic acid
-
___________ is a drug which reduces urination urges by acting as an ________ of the ______ receptors.
Oxybutinin, antagonist, Beta 1 (kidneys)
-
The specific type of adrenergic receptors found in the peripheral blood vessels:__________.
Alpha 1
-
Post-ganglionic neurons of the parasympathetic system release neurotransmitter which binds to cholinergic or ____________ receptors.
muscarinic
-
Can catecholamines be taken orally.
no
-
When a drug is metabolized virtually completely upon passing through the liver, it is called the _________ effect.
First pass
-
A drug for treatment of anaphylactic shock:________.
epinephrine
-
The decongestant that is "behind the counter" in most states is ________.
pseudoephedrine
-
____________is an OTC that is no better than a placebo.
phenylephrine
-
________ was an OTC dietary supplement "stimulant" also used in traditional Chinese medicine ma haung.
Ephedrine
-
Meth abusers often suffer from attack of formication which means______________.
hallucinations of ants crawling on them.
-
_______ and _________ are popular drugs at raves.
MDA (methylenedioxyamphetamine), MDMA (methylenedioxymethamphetamines)
-
Cathinone and methcathinoneare active ingredients in ______ a herb that grows in the Arabian peninsula.
Quat
-
Organic chemists now synthesize similar pure compounds and market them as ________'
Bath salts
-
The major drugs used for ADHD are __________ (generic/trade) and __________ (generic/trade).
methylphenidate(Ritalin), amphetamine
-
Methylphenidate and amphetamines are both_________ drugs.
schedule II
-
A drug used for treating sleep shift disorder and off-label for ADHD and "cognitive enhancement:" _________.
Modafinil
-
The most common fast acting drug for treating asthma, ___________, acts as an ________ of the ___________ receptor.
Albuterol, agonist, Beta 2
-
A few people using this drug experience tachycardia because it also effects their_________ receptor.
Beta 1
-
This drug is most commonly administered with a ________ _______ ________.
MDI, metered dose inhaler.
-
Phase 2 drug metabolism covalently adds a molecule with multiple OH groups called __________ onto drug molecules.
Glucoronic acid
-
The general term for a drug that is actually activated (rather than inactivated) is a ___________.
Pro-drug
-
One specific example of this is ____________.
Codiene
-
A drug with a therapeutic index (TI) of 50 is ________.
Safe
-
A pain medication commonly given transdermally _____________.
Fentanyl
-
A drug for depression with a half life of approximately 1 week is, ___________.
Prozac
-
Babies frequently need a lower drug dosage even after correcting for weight because they do not have fully developed function of the _____ (organ).
Liver
-
A high potency drug ______ always more effacious than a low potency drug.
is not
-
Continued administration of a drug resulting in fewer receptors is an example of ___________.
Pharmacodynamics
-
Continued administration of a drug resulting in increased metabolic enzymes to inactivate the drug is known as _________ tolerance.
Metabolic tolerance
-
Another term for the increase of metabolic enzymes is enzyme_______.
induction
-
An increase in metabolic enzymes results in a ________ in drug efficacy.
decrease
-
A common fruit_____________, contains molecules which inhibit the metabolic isozyme _________.
CYP3A4
-
Two drugs together resulting in more than a simple addictive effect is called a __________ effect.
synergistic
-
The serum protein which binds and transports lipophilic molecules in the blood is called ________.
serum albumen
-
The type of receptor found at the sympathetic ganglia between pre- and post-ganglionic neurons:____________.
Nicotinic
-
The neurotransmitter released by the pre-ganglionic neuron of the sympathetic system:__________.
Acetylcholine
-
The neurotransmitter released by the post-ganglionic neuron of the parasympathetic system is, _____________, and binds to __________ receptors in the affected organs.
Acetylcholine, muscarinic
-
Acetylcholine is inactivated by_______________.
Acetylcholinesterase
-
The primary neurotransmitter released by the adrenal medulla is______________.
epinephrine
-
Epinephrine is inactivated by the enzyme__________ found in high concentrations in the _______(organ).
monoamine oxidase
-
the neurotransmitter whose action is stopped primarily by re-uptake by post-ganglionic neurons is ________________.
norepinephrine
-
A drug used to promote urination after abdominal surgery is_______________.
Bethanecol
-
Sarin, a military nerve gas, works by inhibiting the enzyme ______________.
acetylcholinesterase
-
Sarin gas is quickly lethal to humans by inhibiting the action of the ________(organs).
Lungs (diaphragm)
-
An anticholinergic effect on the pupils is _______.
myodriasis (pupil dilation)
-
An anticholinergic effect on the mouth is _______.
Dry mouth
-
This drug is used pre-operatively to reduce salivation and gi motility.
Atropine
-
Atropine is also used in ambulance to cause _______________.
tachycardia
-
Atropine used to be used to cause ________ in women but is no longer used due to its___________.
Pupil dilation, half life
-
This drug reduces the urge to urinate by acting as an ____________ of the ___________ receptors.
Oxybutynin (Ditropan) or Tolterodine (Detrol), antagonist, cholinergic
-
The most common side effect of Oxybutynin(Ditropan), and Tolterodine (Detrol) is ___________.
Dry mouth
-
The specific type of adrenergic receptor of the heart is _______.
Beta1
-
The specific type of adrenergic receptor found in the lungs is _______.
Beta 2
-
the specific type of adrenergic receptor found in the peripheral blood vessels is ________.
Alpha 1
-
The general term for an adrenergic drug that can not be given orally is ___________.
Catecholamine
-
The Ames test is used to test whether potential drugs are __________.
carcinogenic
-
Phase ____ human trials of a new drug on healthy humans to determine any adverse effects and how quickly it is eliminated from the body.
Phase 1
-
A drug which increases the risk of birth defects is called ____________.
teratogen
-
The drug ____________, was used in the 1950's in Europe for the treatment of morning sickness but resulted in the birth defect __________.
Thalidomide, phocomelia
-
Thalidomide is not used in the treatment of _______ and ________.
leprosy, cancer
-
An x-rated drug, ___________, is still widely used for the treatment of __________.
Accutane, acne
-
______ was widely used to prevent miscarriages in the 50's and 60's, but was discovered to cause health problems in ______.
daughters (DES daughters).
-
use of ibuprofen in pregnant women is not recommended because of increased risk of ______________.
premature closure of the ductus arteriosus
-
The scale of drug addictive potential runs from __ to __.
I to V
-
-
-
-
-
-
-
-
-
-
-
-
-
-
What was Viagra (sildenafil) originally intended for?
hypertensive
-
The generic name for Tylenol is ___________.
acetaminophine
-
Are amines soluble in water?
no
-
If you add acid to an amine group what happens to it?
it becomes an ammonium ion.
-
If you change an amine into an ammonium ion does it become more soluble in water?
yes
-
As acid is added to an amine the pH goes ____, and the ratio of polar/ionic form of the N group _______.
down, decreases
-
If swisherol has a pKa of 9, it will exist primarily as the __________, form in arterial blood.
ionic
-
If hysterical has a pKa of 4 it will exist primarily in the _________ in arterial blood.
polar
-
Drugs will have a maximum efficacy if their pKa is close to _____.
7.4 pH
-
An enzyme family that commonly adds OH groups to drug molecules is called ________.
cytochrome P-450.
-
Specific numbers of this enzyme family are known as _______ or _______.
isoforms, isozyms
-
Name the board that is supposed to ensure the safety of humans in the drug tests.
Institutional review board
-
When a researcher does not do his/her own experimental trials, but redoes the analysis from this trials it is called ___________.
meta-analysis
-
Medical expenses contribute to approx. _____ of personal bankruptcies in the US.
50%
-
A long acting bronchodilator ___________ is most frequently combined with the steroid ___________ as the product __________.
salmeterol, fluticasone, Advair
-
Advair is administered with a ______ _____ _____.
dry powder inhaler
-
What is the adrenergic drug used to stop premature birth.
Terbutaline
-
The alpha 1 antagonist ____________ or ___________, is most commonly used for treatment of __________ ___________ ________.
Doxa' zosin (Cardura), Tamsu' losin (Flomax), Benign Prostate Hypertrophy
-
If medication does not work for BPH what other option do men have?
TURP trans-urethral resection of the prostate
-
___________ is an antagonist to both alpha and beta receptors.
Carvedilol
-
Two specific beta 1 blockers, _________ and _______ are commonly used for treatment of ____________.
Metoprolol, Atenolol, hypertension
-
This CNS active adrenergic antagonist is also available in a patch and can be used for hypertension and withdrawal symptoms.
Clonidine
-
This neuromuscular blocker acts quickly and has a low incidence of vomiting.
succinylcholine
-
Succinylcholine has a mild adverse effect of ______. A more dangerous side effect is ____________ ___________.
Soreness, malignant hyperthermia
-
This neuromuscular blocking agent is put on the arrows of Amazon Indians.
Tubocurarine
-
This partial agonist is used to aid in smoking cessation.
Chantix
-
This seed contains an analog of nicotine and is commonly used as "chew" in Indonesia and other parts of Southeast Asia.
Betel
-
Montelukast (Singulair) is used for the treatment of ____________ and acts by inhibiting the formation of inflammatory molecules called ____________.
asthma, antileukotrienes
-
Teratogen Rating:
Category A
Well controlled testing no significant risk of birth defects.
Levothyroxine
-
Teratogen Rating:
Category B
- Available data in human tests show no evidence of birth defects, inconclusive data though
- amoxicillin
-
Teratogen Rating:
Category C
- adverse effects shown in animal studies, insufficient data on humans. May be prx when benefits outweigh risk.
- ibuprofen (during 1 & 2 trimester, Cat. D 3rd trimester)
-
Teratogen Rating:
Category D
- Clinical data on humans suggests increased risk of birth defects
- Diazepam(Valium), Phenytoin (Dilantin)
-
Teratogen Rating:
Category X
clear evidence of substantial risk of birth defects
Thalidomide
-
Drug Abuse potential:
Control I (Schedule I)
- illegal drugs with no known medical purpose
- phencyclidine (PCP), heroin, GHB, marijuana
-
Drug Abuse Potential:
Control II (Schedule II)
- legal drugs w/ high potential for abuse
- dexroamphetamine (Adderall)
- methylphenidate(Ritalin)
- oxycodone, methadone, hydrocodone, morphine, cocaine.
-
Drug Abuse Potential:
Control III (Schedule III)
- legal drugs with potential for abuse
- codeine + acetaminophen(Tylenol 3), hydrocodone + Tylenol (Vicodin), anabolic steroids, dronabinol(Marinol)
-
Drug Abuse Potential:
Control IV (Schedule IV)
- legal drugs with moderate potential for abuse
- Benzodiazepine sedatives, diazepam(Valium), alprazolam(Xanax), zolpidem(Ambien), eszoplicone(Lunesta)
-
Drug Abuse Potential:
Control V (Schedule V)
- legal drugs w/ lowest potential for abuse
- pregabalin(Lyrica),
-
Which has a longer shelf life polar group or ionic group
ionic
-
Which form of drug works better in a patch
Amine or Ammonium Ion.
Amine, is more lipophilic
-
What blood thinning drug is transported on _________ ________ protein.
Coumadin, serum albumen
-
Metabolism of drugs is done in 2 phases name each phase and the enzyme that is responsible for it.
- Phase I Cytochrome P-450
- Phase II (glucuronyl transferase) adds glucuronic acid.
-
How do Cytochrome P-450, and Glucuronic Acid make drugs easier to metabolize?
They both add OH groups.
-
Define Therapeutic Index.
- LD50/ED50=TI
- LD50=lethal dose in 50% of population
- ED50=Effective dose in 50% of population
- TI should be high, higher the number the safer the drug
-
Bioavailability is a catch all term for how much of the orally administered drug is __________.
absorped
-
If the drug activates the receptors it is known as an _________.
Agonist
-
If the drug inactivates or blocks a receptor it is known as ____________.
antagonist or blocker.
-
If the drug partially activates a drug it is a ______ _______.
If the drug partially inactivates the drug it is a _____________ ____________.
- partial agonist
- partial antagonist
-
Drug Efficacy is _____ _____ a drug is.
how effective
-
When two drugs are taken together and they increase the efficacy of the effects by the sum of their total is known as _______ effect.
addictive
-
When two drugs are taken together and their efficacy is greater than their sum it is known as _________ effect.
synergistic
-
When the liver is stimulated to produce more metabolizing enzymes the result is faster deactivation of the drug and a lower efficacy, this is known as,__________ __________.
Enzyme induction
-
NE is eventually inactivated in the afferent neuron by two enzymes: ______ ______ ( ) and ________ _______ ______ ( ).
- Monoamine oxidase (MAO)
- Catechol Orthomethyl Transferase (COMT)
-
Receptors activated by epinephrine (adrenaline) are known as ________ receptors.
adrenergic
-
Receptors that are activated by acetylcholine are known as __________.
Cholinergic receptors/ muscarinic receptors
-
Epinephrine is inactivated by ______ ______.
monoamine oxidase
-
What are the parasympathetic effects on
eye,
heart
lungs
bladder
Gi tract
genitals
- pupil constricts (near vision)
- HR decreases
- bronchoconstriction
- voiding
- salivation, gi motility
- erection
-
What systems does the sympathetic system affect and their receptors and effect?
- Heart B1, increased hr/contractility
- kidney B1, renin release
- arterioles in heart B2, vasodilation
- bronchi B2, bronchodilation
- uterus B2, relaxation
- Blood Glucose B2, glycogenisis
- peripheral arterioles A1, vasoconstriction
- visceral arterioles A1, vasoconstriction
- eye, A1 pupil dilation
- genitals A1, ejactualtion
-
Bethanecol
- promotes urination, abdominal post-op
- cholinergic(muscarinic) receptors
- agonsit
-
Cholinesterase inhibitors
- increase ACh activity by blocking inactivation of ACh. Causes salivation, bronchoconstriction, continuous stimulation results in muscular and respiratory paralysis, death.
- Sarin Nerve Gas
-
Atropine
- Given Pre-op to decrease salivation and gi motility.
- Causes pupil dilation (Myodriasis)
- long half life
- Bella Donna Plant
-
Tropicamide (Myodriacyl)
- replaced atropine for pupil dilation
- shorter half life
-
ipratropium bromide (Atrovent)
- anticholinergic
- Tx: emphysema, COPD, chronic bronchitis
-
Combivent
ipratropium bromide + albuterol
-
Tiotropium Bromide (Spiriva)
- newer anticholinergic admisnistered by DPI
- longer half life of Combivent
-
Epinephrine
- adrenergic B1, B2, A1 receptors
- use asthma, anaphylactic shock (epipen)
- adjunct in cardiac arrest (causes tachycardia)
- can't be given orally
-
Norepinephrine
adrenergic receptors except B2
-
Pseudoephedrine (Sudafed)
- non-catecholamine
- A1, B1, B2
- A1 nasal vasoconstriction
- used to make methamphetamine
-
Phenylephrine (Sudafed-PE)
- replacing pseudoephedrine
- studies suggest not any better than placebo
-
Ephedrine
- isomer of pseudoephedrine
- found in Chinese herb Mahuang
- several deaths contributed to it
-
Amphetamine(Benzedrine)
(methylamphetamine)
synthetic analogues of epinephrine
-
Meth abuser's suffer from an oral condition referred to as ______ ______.
meth mouth
-
Meth abusers often hallucinate about bugs crawling on them this is known as ____________.
formication
-
This drug is known as the mellow drug of America.
- MDA, methylenedioxyamphetamine
- produces a energy rush and self-awareness
- popular at raves
- Schedule I
-
This drug is knows as ecstasy or molley.
- MDMA methylenedioxymethamphetamine
- may change serotonin receptors
- Adverse effects:
- tachycardia, hyperthermia
- (sometime results in coma and death)
- Schedule I
-
Quat
- shrub grown in Arabian peninsula
- adrenergic agonist
- cathinone
- (non-catecholamine)
-
Bath Salts
synthetic derivatives of cathinone
-
Methylphenidate (Ritalin)
- used for Tx of ADHD
- inhibits uptake of dopamine and NE
- Schedule II
-
Dexmethylphenedate (Focalin)
right hand glove of methylphenidate
-
Amphetamine (Adderall)
Control II also used for tx of ADHD
-
Modafinil (Provigil)
- approved for Tx of narcolepsy, shift work sleep disorder, inc. release of monoamines like epinephrine and NE.
- cognitive enhancement (off-label)
-
Beta 2 agonist cause
- bronchodilation
- uterine relaxation
- glycogenolysis
-
MDI or DPI
- metered dose inhaler
- dry powder inhaler
-
Inhalers used to use _____________ they now are using _____________.
- chlorofluorcarbons (CFC's)
- hydrofluoralkines (HFA)
-
Albuterol or Salmeterol
- B2 agonist
- 5-15 min. onset
- rescue inhaler
-
Salmeterol
- long lasting agonist B2
- used in combination w/ Fluticasone
-
Terbutaline
- prevention of premature parturition
- B2 agonist
-
Doxa' zosin (Cardura)
- used in treatment of BPH
- originally used for hypertension
- AE: orthostatic hypotension, nasal congestion, inability to ejaculate
-
Tamsu' losin (Flomax)
used in tx of BPH
-
Define BPH
Benign Prostate Hypertrophy
-
Define TURP
Tran-urethral resection of the Prostate
-
Carvedilol
- non-specific adrenergic blocker
- causes: decrease hr. Peripheral vasodilation
- should not be used in respiratory problems
-
Propranolol
- B1/B2 blocker
- decr. Hr, and intensity
- may cause vasoconstriction
-
Metoprolol
- Specific B1 blocker
- bid
- Toprolol qd
- commonly used antihypertensive drug, prevent tachycardia (bad for diabetics)
-
Atenolol
- B1 blocker
- qd
- long term use of Atenolol inc. risk of T-2 diabetes.
-
Clonidine
- Tx for blocks CNs receptors
- is available in patch form(only antihypertensive in patch form) adjunct for tx of ADHD
- decreases HR
- AE: dry mouth
- drowsiness
- teratogen
-
Tubocurarine
neuromuscular blocker in curare, used on arrow in South America
-
L-Dopa/carbidopa
- used in treatment of Parkinsons Disease
- slows down metabolism of Dopamine
-
DOPA decarboxylase
- metabolizes L-DOPA into dopamine,
- dopamine can not be given orally ( first pass effect)
-
Parkinsons Disease Meds
- Pramipexole (Mirapex)
- AE: somnolence, sudden sleep attacks
-
Selegiline (Eldepryl, Deprenyl)
inhibits type B monoamine oxidase
-
Topiramate (Topomax)
- inhibits NA+ channels, FDA approved fro migraines, off-label use for neuropathic pain
- TX: partial complex seizures
-
Carbama'zepine (Tegretol)
- NA+ channel blocker
- tx: Grand Mal and complex seizures, not Absence Seizures
- efficacy in Bi-polar disease and neuralgia
- (stimulates production of Cytochrome P-450)
- decrease efficacy
- AE: sedation, ataxia, agranulocytosis, Cat C., Steve Johnson syndrome
-
Oxcarbazepine
- tx for grand mal &comlex seizuresSimilar to Carbamazepine
- does not have risk of agranulocytosis or aplatic anemia(bone marrow loss)
-
Phenobarbital
- works on GABA receptors
- effective against all seizures except Absence seizures
- Cat D teratogen (probable)
- AE: sedation, lethargy, CNS depression(respiratory depression)
-
Valproic Acid (Depakane)
- Only seizure medicine to work on ALL types of seizures (including Absence seizures).
- Has hi rate of nausea, vomiting. Divalproex enteric coated Depakane reduces vomiting
- AE: nausea, vomiting, hepatoxicity, teratogenicity (Cat. D)
-
Lamotrigine (Lamictal)
- NA+ channel blocker
- primarily used for partial seizures and tonic-clonic
- mood stabilizer in Bi-polar disorder
- AE: ataxia, headache, nausea, rarely Steven Johnson syndrome.
-
Levetiracetam (Keppra)
adjunct drug in tx of partial and tonic-clonic seizures
-
Benzodiazepines for seizures
Lorazepam(Ativan)
Diazepam(Valium)
both commonly used for tx of status epilepticus, given IV or rectal
-
Benzodiazepines for seizures
Clonazepam (klonopin)
commonly used in tx of absence seizures
-
Benzodiazepines for seizures
Gabapentin (Neurotin)
- antagonist to CNS, inhibits NA+ channels in the brain
- adjunct therapy in partial and secondary generalized seizures
- large TI
- AE: sedation ataxia
-
Benzodiazepines for seizures
Pregabalin(Lyrica)
- newer version of gabapentin
- tx of partial seizures, neurological pain assoc. with diabetes and shingles
- FDA approved for tx of Fibromyalgia
-
Alternative TX for Seizures
- Extreme ketogenic diets, high fat low carb diet
- reduces seizures usually in children.
- Vagus nerve stimulation- stimulation of vagus nerve for 30 sec. every 5 min. reduces freq. and severity of seizures.
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