MD PHARMACOLOGY Flashcards
1
Q
WHAT ORGAN METABOLIZES AMIDES?
EX OF AMIDES
A
LIVER
BLAMP
- bupivicaine
- lidocaine
- ariticaine
- mepivicaine
- prilocaine
2
Q
WHAT METABOLIZES ESTERS?
EX OF ESTERS?
A
Pseudocholinesterase in PLASMA
procaine (not prilocaine)
benzocaine
tetracaine
cocaine
3
Q
which amide is the safest in children?
lidocaine
bupivicaine
mepivicaine
articaine
pilocaine
A
LIDOCAINE
also has shortest duration of action on the list = inc blood flow = less potent = less lipid soluble
4
Q
which amide causes least vasodilation?
lidocaine
bupivicaine
mepivicaine
articaine
pilocaine
A
mepivicaine
5
Q
which amide is NOT safe in children ?
lidocaine
bupivicaine
mepivicaine
articaine
pilocaine
A
BUPIVICAINE ( longest duration)
6
Q
Which local anesthetic causes METHEMGLOBINEMIA?
prilocaine
lidocaine
mepivicaine
bupivicaine
A
PRILOCAINE
7
Q
lognest duration ?
lidocaine
bupivicaine
mepivicaine
articaine
pilocaine
A
bupivicaine ( not child safe)
longest duration = highest PKA
8
Q
which amide has longest duration? **
lidocaine
bupivicaine
mepivicaine
articaine
pilocaine
A
BUPIVICAINE
mepiv: 7.6
lido,prilo,arti 7.8
bupiv: 8.1
higher the potency = longer duration of action = higher lipid solubility
9
Q
TOPICAL ANESTHETIC IS ESTER OR AMIDE? what is the name of it?
A
ESTER
BENZOCAINE
10
Q
pharmacodynamics of LA causes what in ion channels?
A
SODIUM CHANNEL BLOCKER
11
Q
which has the highest pka of LA?
mepivicaine
lidocaine
prilocaine
articaine
bupivicaine
A
mepivicaine: 7.6 ( more rapid onset)
lido, prilo, arti : 7.8
bupiv: 8.1 (longer duration)
lower pka = stronger the acid = faster onset of action
12
Q
how much liquid in carpule?
A
1.8 mL
13
Q
2% lidocaine has how many mg of lidocaine per carpule ?
board**
A
2 x 18 mg = 36 mg per carp
14
Q
3 fxns of vasoconstrictors?
- effects on numbness?
- effect on toxicity?
- effects on hemostasis?
A
prolong numbness
reduce toxicity (flushes out)
promote hemostasis
15
Q
max epi dose for ASA 1 patient
A
.2 mg
16
Q
max epi dose for cardiax patient
A
.04 mg
17
Q
max lido dose without vasoconstrictor
A
4.4 mg/kg
18
Q
max lido dose of LA with vasoconstrictor
A
7 mg/ kg
19
Q
PROPER WAY TO DELIVER LA?
A
slow: 1 carpule/ min
20
Q
length of long needle? **
A
32 mm
21
Q
length of short needle ? **
A
20 mm
22
Q
which guage needle has better aspiration?
27
15
25
30
A
30 !!! ( smaller hole)
23
Q
width of 30, 27, 25 gauge?
A
30- .3mm
27 - .4 mm
25 - .5 mm
24
Q
how much of the carpule for IA nerve block?
A
3/4
25
how much carpule of Buccal nerve block?
1/4 carpule
26
where is mental nerve block given and how much of carpule?
apices of PM
1/3
27
which nerve block do you have to apply 3 minute pressure so it works?
INCISIVE nerve block
28
THIS BLOCK HAS HIGHEST HEMATOMA RISK?
PSA
29
HOW DEEP FOR PSA ?
16 MM ( HALF LENFTH OF LONG NEEDLE)
30
THIS IS CALLED THE TRUE ASA BLOCK
IO BLOCK
31
WHICH IS MOST PAINFUL BLOCK?
NP
32
WHAT LA IS BEST FOR LOCAL INFILTRATION?
**_ARTICAINE_** (SEPTOCAINE) BECAUSE BEST BONE PENETRATION
33
SULFONAMIDES MECHANISM OF ACTION ??
SULFONAMIDES
FOLATE SYNTHESIS INHIBITOR : inhibit incorporation of **_PABA_** into _folic acid_,
sulfadiazine ; sulfamethoxazole
34
which calss of drugs is a folate synthesis inhibitor?
sulfamides
35
FLUOROQUINOLONES:
mechanism of axn
cidal or static\>
examples ?
DNA synthesis inhibtor
cidal
cipro**_flaxocin_** ; levo_floxacin_
36
Penicillin:
bactericidal or static?
mechanism of penicillin?
molecular structure?
BOARD \*\*\*\*\*
bactericidal
cell wall synthesis inhibitor
**B-Lactam ring**
37
Penicillin is cross allergenic with what?
CEPHALOSPORINS (chemically related; allergic to this if allergic to penicillin)
38
which type of penicillin is taken orally ?
BOARD \*\*\*
PENICILLIN V
39
which penicillin is taken by IV sedation ?
BOARD \*\*\*
PEN G !
**IV** RHYMES WITH **G**!!
40
what is AUGMENTIN?
**_PENICILLIN_** !!!!
combo of
AMOXICILLIN
+
CLAVULANIC ACID (_***b -lactamase- resistant***)_
clavulanic acid= stops breakdown of penicillin b-lactam ring !!!
41
WHICH PENICILLIN BEST AND BROADEST?
augmentin
ampicillin
penicillin V
Methicillin
amoxicillin
AMPICILLIN
best and broadest g- spectrum !!!
42
a patient who is allergic to cepphalosporin should never be given this
PENICILLIN ( chemically related)
43
CEPHALOSPORIN:
cidal or static?
what is the mechanism?
examples
bactericidal
**cell wall synthesis, B-lactam ( same as penicillin)**
Cephalexin, cefuroxin, ceftriaxone, ceftriaxone, cefepime
cephala same as penicillin
**anything with _CEF_ or _CEPH_ !!**
44
ANTIBIOTIC WITH BROADEST SPECTRUM\*\*
tetracycline
macrolide
lincosamides
tetracycline
45
TETRACYCLINE:
static or cidal?
mechanism ?
examples ?
PROTEIN SYNTHESIS INHIBITOR
(**30S** ribosomal subunit)
static
tetracycline doxycycline minocycline
46
TETRACYCLINE DRUGS
TETRACYCLINE
DOXYCYCLINE
MINOCYCLINE
47
**MACROLIDES**:
static or cidal
mechanism
types
**STATIC** \*\*
Protein Synthesis inhibtor ( 50 S )
Eryhthro**mycin**
Clarithro**mycin**
Azithro**mycin**
MAC LIKED TO THROW MICE
48
First choice for INFECTIOUS ENDOCARDITIS prophy?
amoxicillin 2g ( 1 hr before)
49
LINCOSAMIDES:
static or cidal ?
mechanism ?
types?
**STATIC**
PROTEIN SYNTH INHIBITOR (50S)
CLINDAMYCIN
LINCOMYCIN
**_LINK_ ALSO _HIDES MICE_**
50
MACROLIDES VS LINCOSAMIDES
static or cidal?
mechanism ?
examples?
STATIC
Protein Synthesis inhibtor ( 50 S )
Eryhthromycin
Clarithromycin
Azithromycin
***MAC*** is from ***AZ***; ***Clari*** from ***Eryth***
STATIC
PROTEIN SYNTH INHIBITOR (50S)
CLINDA**MYCIN**
LINCO**MYCIN**
***Linco*** says ***LInc*** rearranged is ***Clin***
51
WHEN IS AB PROPHYLAXIS NECESSARY IN CARDIOVASCULAR CONDITIONS?
4 reasons
BOARD \*\*\*
* **prosthetic heart valve**
* history of endocarditis
* heart transplant with VALVULOPATHY/ VALVE DYSFUNCTION
* CONGENITAL HEART PROBLEMS
52
WHEN IS AB PROPHYLAXIS REQUIRED IN COMPROMISED IMMUNITY?
3 reasons
ORGAN TRANSPLANT
NEUTROPENIA
CANCER THERAPY
53
First choice for INFECTIOUS ENDOCARDITIS prophy in children?
antibiotic type?
dosage?
**amox 50mg/kg** 1 hr before
54
INFECTIOUS ENDOCARDITIS prophy with penicillin alergy ?
**CLINDAMYCIN 600 mg** 1Hr before
55
RX FOR PROSTHETIC JOINT PROPHYLAXIS and dosage?
clindamycin
amoxicillin
keflex
ampicilin
KEFLEX 2G (1 hr before)
56
mitral valve AB prophy ?
none!!
mitral valve prolapse isnt necessary for AB
neither is
cardiac pacemaker
rhematic fever w/out valvular dysfunction
mitral valve prolape w/out valvular regurgitation
57
This antibiotic causes PSEUDOMONAS COLITIS?
clindamycin
tetracycline
macrolides
lincosamides
CLINDAMYCIN
causes GI issues !!!
58
PSEUDOMONAS COLITIS CAUSED FROM WHAT DRUG?
CLINDAMYCIN
inflammation of colon
59
what type of drug causes SUPERINFECTION?
Broad spectrum AB ! (kill good and bad bacteria)
- **TETRACYCLINES ( doxy, mino)**
**- AMPICILLIN**
**- augmentin**
60
what AB is associated with APLASTIC ANEMIA?
tetracycline
chloramphenicol
ampicillin
erythromycin
CHLORAMPHENICOL
61
what types of antibiotics cause LIVER DAMAGE? \*\*
erythomycin
chloramphenicol
tetracycline
clindamycin
TETRACYCLINE
62
This antibiotic associated with allergic cholestatic hepatitis ?
clindamycin
chloramphenicol
tetracycline
erythomycin
ERYTHOMYCIN ESTOLATE
63
A patient walks in and is on birth control, what type of medication should you not prescrive for infection?
ANTIBIOTICS ( cancel out)
64
what happens when give bacteriaxidal and bacteriasttic drug?
cancel out !
65
WHERE IS CLINDAMYCIN CONCENTRATED IN THE BODY?
BONE
66
HERE IS TETRACYLINE CONCENTRATED IN THE BODY?
GCF (that is why used in perio tmnt)
67
WHAT DO YOU USE TO TREAT HERPES?
ACYCLOVIR / VALCYCLOVIR
68
what do you use for CANDIDIASIS?
FLUCON**AZOLE**
KETOCON**AZOLE**
69
FLUCONAZOLE USED TO TREAT WHAT?
CANDIDIASIS
70
What is the drug that you give to treat **_candidiasis_** in trochea form ?
CLOTRIM**_AZOLE_** !!!
71
MECHANISM OF ASPIRIN (ASA)
COX 1 AND 2 BLOCKER ( irreversible)
72
MECHANISM OF IBUPROFEN?
COX 1 AND 2 BLOCKER (reversible)
aspirin: **irrevirsible**
ibuprofen: **reversible**
73
WHAT NSAID CAUSES GI ISSUES?
ibuprofen
asprin
celebrex
naproxen
ASPIRIN
74
WHAT NSAID CAUSES **_KIDNEY_** ISSUES?
aspirin
ibuprofen
celebrex
aleve
IBUPROFEN
75
WHAT IS WORSE COX 2 OR 1
COX 2
76
NSAIDS MECHANISM OF AXN
BLOCK COX 1 AND 2
77
What does each drug effect?
aspirin
ibuprofen
acetaminophen
aspirin: GI
Ibuprofen: kidney
Acet: liver
78
WHAT IS THE DRUG OF COICE FOR CHILD WITH FEVER?
aspirin
acetiminophen
ibuprofen
ACETIMINOPHEN
(childrens tylenol)
79
what disease can develop when a feverish child is givin aspirin?
**REYES SYNDROME**
(encephalopathy; hepatic dysfunction)
80
wWHAT DRUG IS HEPATOTOXIC
ACTAMINOPHEN
81
flucanazole is used to treat what?
candidiasis (anti fungal)
-azole
82
A PATIENT HAS KINDEY DISEASE, WHAT MED SHOULD HE TAKE ?
ACETIMINOPHEN
83
PATIENT HAS LIVER DISEASE, WHAT MED SHOULD HE TAKE?
tylenol
ibuprofen
aspirin
IBUPROFEN
84
MAXIMUM DOSE OF IBUPROFEN
3.2 G/DAY
85
max dose of acetiminophen ?
4g / day
86
mechanism aspirin as analgesia?
INHIBITS COX 1 AND 2
## Footnote
**( inhibits PG syntehsis)**
87
HOW DOES ASPIRIN WORK AS AN ANTIPYRETIC ?
inhibits **PG syntehsis** in **HYPOTHALMUS**
88
MECHANISM OF HOW ASPIRIN EFFECTS BLEEDING TIME?
inhibits TXA2 SYNTHESIS which inhibits PLATELET AGGREGATION
89
MECHANISM OF ASPIRIN:
ANALGESIC
ANTIPYRETIC
BLEEDING TIME
MOST IMPORTANT SLIIDE !!
**inhibits** Cox 1 (AA) and 2 (**PG syntehsis**)
i**nhibits PG syntehsis** in ***_Hypothalmus_***
inhibits **thromboxin (A2)** synthesis inhibits *_platelet aggregation_*
PG = INFLAMMATION
ANTIPYRETIC = TEMPERATURE (hypothalmus)
bleeding time: thomboxane 2 syntehsis
90
CORTICOSTEROID:
how many rings?
4 ring structe
91
MECHANISM OF STEROIDS?
Analgesic
inhibits phospholipas A2 (AA syntehsis) turns to prostoglandis
92
biggest side effect of taking **_steroids?_** \*\*\*\*
**ADRENAL INSUFFICIENCY**
rule of 2, adrenal insufficiency can happen if :
**20 mg / 2 weeks/ 2 years** ( take 20 mg of cortisone for 2 weeks within 2 years of tmnt)
93
what receptoirs do narcotics/ opiod affect ?
Mu-opioid receptor **_agonists_** (in CNS)
94
which narcotic has controlled release ?
morphine
hydrocodone
oxycodon
codeine
heroin
oxycontin / oxycodone
95
Drug combination of **_Vicodin_**?
HYDROCODONE + ACETAMINOPHEN
96
what drugs combine to form **_percocet_**?
OXYCODONE (stronger) + ACETAMINOPHEN
97
TYLENOL 2 COMBINATION AND DOSAGE\>
300 mg ACET + 15 mg codenine
98
TYLEONL 1 COMBO?
300 mg ACET + 8mg codeine
99
TYLENOL 3 COMBO?
300 mg ACET + 30 mg CODEINE
100
TYLENOL 4 COMBO?
300 mg acet + 60 mg codeine
101
TYLENOL 1,2,3,4 COMBO?
* 300 / 8
* 300/ 15
* 300/ 30
* 300 / 60
102
SIDE EFFECTS OF MORPHINE \*\*\*
Spells out MORPHINE
**MIOSIS**
OUT OF IT
\*\*\* RESPIRATORY DEPRESSION\*\*\*\*
PNEUMONIA
HYPOTENSION
INFREQUENCY
NASUSEA
EUPHORIA AND DYSPHORIA (happy and sad)
103
TREAT ADDICTION USING WHAT?
METHADONE
104
sensation before and after nitrous oxide
tingling
naseua
105
peripheral neuropathy is caused by what?
long term exposure to **_nitrous oxide_**
causes weakness, numbness and pain, usually in your hands and feet.
106
minimal alveolar concentration of nitrous oxide?
105%
107
WHAT HAPPENS TO LUNGS WHEN NITROUS OXIDE TURNED OFF
DIFFUSION HYPOXIA
108
PHARMACOKINETS STEPS?
0 administration
1 absorption
2 distriubtion
3 metabolism
4 elimination
109
HOW IS INSULIN DELIVERED?
oral
sublingual
subcutaneous
IM
IV
SUBCUTANEOUS (under skin)
110
how is epi pen delivered?
IM
IV
Subcutaneous
IM ( in muscles)
111
how is nitroglycerin delivered?
sublingually
112
most common method of drug administration?
IV
IM
Inhalation
Oral
subcutaneous
ORAL
113
ABSORPTION:
How do drugs get into body?
_Local Drugs:_ cross cell membrane (epithelium) through **PASSIVE DIFFUSION** (must be non-ionized) into bloodstream (endothelium)
_Systemic : straight to blood stream_
114
WHAT IS BIOAVAILABILITY?
fraction of dosage that reaches system
115
PH and PKA of drugs
weak acids: pH \< PKA
weak bases: pH \> pka
acid environment/ acidic drug: **NON IONIZED**
basic environment/ basic drug: **NON IONIZED**
non ionized: what we want, moves freely across membrane
116
where does drug have to get in order to be distriburted effectively?
BLOOD
117
DESCRIBE **_FIRST PASS EFFECT_**
ORAL drugs go through LIVER reduces bioavailability
118
distribution of drugs across 3 bodies of water in the body?
40%: intracellular
16%: Interstitiial
**4%: Plasma**
119
who has more body water. obese or normal?
normal !
120
what part of body uses most and least water?
most: BRAIN AND MUSCLE
least: ADIPOSE
121
describe phase I and phase II of metabolism of drugs \*\*\*\*\*
drug -\>phase I metabolite -\> phase II inactive
**_PHASE I:_**
fxn: oxidation, reduction, hydrolysis
***CYTOCHROME P450***
**_PHASE II:_**
conjugation ( joining of group): glucouronide, glutathione, glycine
***UDP-GLUCOURONOSYTRANSFERASE***
122
DESCRIBE ELIMINATION PROCESS OF DRUG
PHASE 1: PEE ( polar)
PHASE II: poop (nonpolar)
123
constant amount of drug elinmintated per unit of time is what?
0 order kinetics
1st order kinetics
2nd order kinetics
ZERO:
doesnt matter amount drug taken b/c same amount elinated per hr
mg/hr
124
constant fraction of drug elinmintated per unit of time is what?
0 order kinetics
1st order kinetics
2nd order kinetics
FIRST ORDER
% of drug per hour thats eliminated
%/hr
125
higher risk of drug accumulation
zero order or first order
ZERO ORDER
fraction of drug
126
what is the process called when a drug is inducing liver cytochrome enzyme does what to drug #2?
**INDUCTION**
**reduces effect**
127
what is it called when drug #1 **_competes_** for metabolism or directly inhibits liver cytochrome.
what does this do to drug 2?
**INHIBITION**
increased toxicity !!
128
pharmacokientics vs pharmacodinamics ?
kinetics:
absorption / distribution / metabolism / clearance
dynamics:
drug receptor interction
129
almost all drug targets are what ??
**_PROTEINS !!_**
receptors
ion channels
enxymes carriers
130
a substance which initiates a physiological response when combined with a receptor.
AGONIST
131
full vs partial agonist
partial: cant produce 100% of desired effect
Full: can produce 100% of desired effect
132
inhibits normal function of endogenous agonist
antagonist
133
competitive vs noncompetitive antagonist?
**comp:** competes for same binding site on receptor
**non-comp**: binds to differnet binding site and _changes morphology_ which prevents from binding
134
INVERSE AGONIST inhibits what?
define it
**_BASAL ACTIVITY_**
drug that binds to the same receptor as an agonist but induces a pharmacological **response opposite** to that of the agonist.
135
TYPE 1 DOSE RESPONSE CURVE:
X axis?
Y acis?
**CURVE TYPE?**
x- dose of drug
y- response/ efficacy of drug
hyperbolic or **SIGMOID/ LOG FORM**
136
TYPE 1 DOSE RSPONSE CURVEL
what is intrinsic activity?
MAXIMAL EFFECT OF DRUG (**EMAX**) (full agonist )
full agonist: intrinsic of 1
partial agonist 0-1
antagonist = )
137
TYPE 1 DOSE CURVE:
what is efficacy?
effect of a drug as a function of bonding
138
TYPE 1 DOSE CURVE:
what is affinity?
attractiveness of drug to receptor
LOWER the dissaosication constant (**kd**) = HIGHER the affinity
139
DIFFERNECE BETWEEN PENEICILLING G AND V ?
\*\*\*\*\* important !!!
PEN G : more sensitive to acid degredation !!!!!
some PEN V preferred
140
WHICH PENICILLIN BROADEST SPECTRUM ??
AMPICILLIN
CARBENICILLIN
METHICILLIN
AUGMENTIN
AMPICILLIN (preferred for G-)
141
WHICH PENICILLIN IM OR IV ??
AMPICILLIN
CARBENICILLIN
METHICILLIN
AUGMENTIN
AMPICILLIN 2G
142
HOW IS POTENCY MEASURED ?
EC50 : affective conventration of drug leading to half its minimal effect
MORE POTENT = LOWER EC50
143
competitivt antagonist shifts agonist curve which way?
RIGHT !!!
144
NONCOMPETITIVE GONIST SHIFTS AGONIST CURVE WHICH WAY?
DOWN
145
COMPETEITIVE VS NONCPM[ETOTOVE ANTAGONIST AND HOW SHIFTS AGONIST CURVE?
competitive: RIGHT
noncomepetitive: DOWN
adding competitive antagonist = drags curve right ( need more drug to produce response)
146
TYPE II DOSE RSPONSE CURVER
X AND Y AXIS?
X: DOSE OF DRUG
Y: # OF SUBJECTS RESPONDING TO DRUG (rather than efficacy like type I curve)
147
TYPE II :
ED50 ?
TD 50?
LD 50 ?
ED: **effective** dose; 50% population rseponded effectively (treated)
TD50: **toxic** dose: 50 % population experienced toxic side effects
LD50: **lethal** dose; 50% population responded lethally (died)
148
type I vs TYPE 2 DOSE response curves !!! what do they measure?
type 1: dose v efficacy of drug
type II: dose vs reponse of patient
149
WHEN TALKING ABOUT DRUGS WHAT IS **ADDITIVE** EFFECT?
combining drugs COMBINES their effect
150
what is an antagonistic drug?
combining drugs causes lesser effect than each one alone
151
what is synergistic in drugs?
combining drug leads to MORE THAN THE SUM of 2 independelty !!
152
ANS PHARMACOLOGY:
which drugs affect PSNS?
which drugs affect SNS?
IMPORTATNT !!!!!!
PSNS: **cholinergic**
sns: **adrenergic**
153
SNS VS PSNS HOW THEY AFFECT:
pupils
saliva
HR
airway
digestion
bladder
**rest and digest** (feed and breed) :
constriction
stimulate saliva
dec HR
airway constriction
stimulate digestion
**bladder constriction**
154
RECEPTORS IN ANS:
IONOTROPIC VS METABOTROPIC
ION: ION CHANNELS (once open allows ions to pass thru)
METABOTROPIC: G-PROTEIN COUPLES RECEPTORS ( acitvates 2nd messenger)
155
RECEPTORS IN ANS :
CHOLINERGENIC VS ADRENERGENIC \*\*\*\*\*\*
what do they bind ?
**_CHOLINERGENIC_**: binds **acetycholine**
- NICOTONIC : binds nicotine; ionotropic
- MUSCURANIC: binds muscarine; metabotropic
**_ADRENERGIC_**: binds **EPI/NE;** ***metabotropic*** (always)
156
CHOLINERGENIC
2 RECEPTORS?
NICOTINIC
MUSCURINIC
157
ADRENERGENIC RECEPTORS
what does it bind?
metabotropic or ionotropic?
binds epi/ ne
METABOTROPIC ( g cpuples recetor)
158
RECEPTORS IN THE ANS
159
SNS VS PSNS BY REGION OF SPINAL CORD:
**PSNS** : CRANIO/SACRAL **CS**
**SNS**: THORACO/LUMBAR **TL**
160
SNS VS PSNS BY LEGNTHS OF PRE AND POST GANGLIONIC NERVES
PSNS: long pre; short post
SNS: short pre; long post
161
SNS VS PSNS neurotransmitters they use :
**PSNS**: AcH everywehre
**SNS**: AcH to *ganglion* NE from *nerves*; EPi/NE from *adrenal gland*
162
ANS:
SNS VS PSNS neurotransmitters they use \*\*\*\*
PSNS: muscarinic metabotropic
SNS: adrenergenic metabotropic
163
HOW IS THE SYNTHESIS RXN OF ACETYLCHOLINE ?
**Acetyl** CoA + **choline**= ACETYLCHOLINE
catalyzed by choline acetyltransferase
reversed by acetylcholine**_esterase_**
164
WHAT DO THESE MUSCURANIC RECEPTORS AFFECTS?
M1
M2
M3
M4
M5
M1, M4, M5: CNS
M2: heart
M3: Smooth muscle
165
MUSCURANIC RECEPTOR
PSNS or SNS?
PSNS
rest and digest
166
function oF M2 AND M3 MUSCURANIC RECEPTORS?
RMBR, MUSCURANIC IS PSNS = REST AND DIGEST !!!
M2= HEART; **BRADYCARDIA**
M3= SM; **SLUDS** / **BAM**
***SLUDS***: salivation, lachrymation, urination, defecation, sweating
***BAM***: brnchoconstriction, ab cramps, **_miosis_** ( constritction)
167
M AGONIST AFFECTS WHICH M RECEPTOR?
NON-SELECTIVE (SO AFFECTS ALLA SM1-M5)
168
WHAT IS THE ISSUE WITH M AGONISTS \>
**non selective ( works all M receptors)**
dont use on:
- peptic ulcers (***gastric acid***)
- asthma/ COPD (***bronchconstriction***)
- CHF (***dec. cardiac output***)
169
M AGONIST USED FOR STUMULATING SALIVA OR EYE DROPS ?
**PILOCARPINE** (constricts pupils)
glaucoma and salivary production
170
what are the 2 **_DIRECT_** acting **M agonists**
**PILOCARPINE**
**METHACHOLINE**
remember. these are M agonists so they work on PSNS. agonist affet heart, SM , CNS
171
WHAT ARE THE FXN OF **INDIRECT ACTING M AGONISTS**?
INHIBIT **ACETYLCHOLINEE**_STERASE_****!
stops breakdown of aCh
172
THIS **INDIRECT-ACTING DRUG** _RESERSIBLY_ INHIBITS CHOLINESTERASE
**NEOSTIGMINE**
Inhibits the hydrolysis of acetylcholine by competing with acetylcholine for attachment to acetylcholinesterase at sites of cholinergic transmission
173
IRREVERSIBLY INHIBITS CHOLINESESTERASE
**ORGANOPHOSPHATE INSECTICE**
potent and poisonous
174
ORGANOPHOPSHATE INSECTICIDE POISONING CAN BE TREATED WITH ? \*\*
PRALIDOXAMINE
175
DIRECT ACTING VS INDIRECT ACTING M AGONIST \*\*\*
what they fxn?
drugs in each?
**_DIRECT_**: activates M receptor; *_mimics ACH_*
- **pilocarpine** (saliva; constrict)
- **methacholine**
**_INDIRECT_**: non competitively *_inhibits cholinesterase_*
- **neostigmine** (**reversibly** inhibts cholinesterase)
- **organophosphate** insecticide (**irreversibly** inhibits cholinesterase )
176
WHICH DRUG REDUCES SALIVA OR EMERGENCY DRUG TO TREAT BRACHYCARDIA ( CAN ALSO CAUSE TACHYCARDIA)
**ATROPINE**!!!
m antagonist/ antimuscarinic!!! ( opposite of psns)
opposite drug: pilocarpine
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WHAT IS ATROPINE?
m antagonist/ antimuscarinic!!! ( opposite of psns)
OPPOSITE OF PILOCARPINE
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MECAMYLAMINE
fxn?
what class of drug is it whats it due to receptors?
***ANTIHYPERTENTSIVE***
N ANTAGONIST/ GANGLIONIC BLOCKERS
**non polarizing!!**
**_blocks N receptor at allosteric site_** (site that allows molecules to inhibit or turn on enzyme activity)
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THIS N ANTAGONIST is a ganglionic blocker that used to treat extreme hypertensive patients.
MECAMYLAMINE
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THIS DRUG IS AN N ANTAGONIST/GANGLIONIC BLOCKER THAT BINDS TO N RECEPTOR BUT CANT BE REMOVED
NICOTINE !!!
**DEPOLARIZING**: binds N receptor and cant be moved
in image: Na+ causes DEPOLARIZATION allows nicotine in and binds to N receptor
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THIS DRUG IS FOUND IN ARROW POISON:
name?
drug class/ type?
**TUBOCURARINE**
N-_antagonist_/ neuromuscular blocker
non-depolarizing ; blocks N receptor at active site
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THIS DRUG PREVENTS LARYNGOSPASMS AND SKELETAL MUSCLE RELAXANT
SUCCINYLCHOLINE
Depolarizing: binds N receptor but cant be removed
n antagonist/ neuromuscular blocker
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M RECEPTORS and N RECEPTORS OVERVIEW !!!! \*\*\*\*
IMPORTANT !!!!
**_M AGONIST:_**
***direct acting; activates M receptor (mimics ACh)***
PILOCARPINE
METHACOLINE
***indirect -acting; non competitbely inhibits acH-esterase***
NEOSTIGMINE: reversibly inhibits ach-esterase
ORG PHOSPHATE INSECTICIDE: irreversibly inhibits cholinsterase
**_M ANTAGONIST/ ANTIMUSCARINIC:_**
***competitive inhibitors; block N receptors compete with ACh***
Atropine: dec. saliva/treat bradychard (cause tachy)
\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
**_N ANTAGONIST: GANG BLOCKERS_**
***non-depolarizing; blocks N receptors at allosteric sites***
MECAMYLAMINE: antihypertensive
***Depolarizing; binds N receptor but cant be removed***
NICOTINE
**_N ANTAGONIST/NEUROMUSCULAR BLOCK:_**
***non-depolarizing/blocks n recetor at active site***
TUBOCURARINE: arrow poison
***depolar. binds to N receptor but cant be removed***
SUCCINYLCHOLINE: skeletal muscle relax
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STEPS OF EPINEPHRINE AND NE SYNTHESIS
TYROSINE -\> L-DOPA -\> DOPAMINE -\> NE -\> EPI
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CATECHOLAMINES VS MONAMINES ?
CATECH : Dopamine, NE, EPI
MONAMINES: catecholamines + serotonin (5-HT) and histamine
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**WHAT ARE THE 4 ADRENERGENIC RECEPTORS AND WHAT PART OF BODY DO THEY AFFECT? \*\***
a1: **SM** (vasculature)
a2: **SM**
B1: **Heart** (sa/av node)
B2: **SM** ( albuterol)
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which adrenergenic receptors affect the heart?
B1
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which adrenergic receptors affect SM?
a1
a2
B2
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**what do _a-receptors_ do:**
blood pressure
urinary system
pupils
VCONSTRICTION
URINARY RETENTION
**D**ILATION (MY**D**RIASIS)
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WHAT DOES a -1 vs a-2 receptors do?
a-1 :
vasoconstriction
urinary retention
dilation (mydriasis)
a-2:
vconstriction
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B1 VS B2 RECEPTORS:
**_B1: FIGHT OR FLIGHT (SNS)_**
- tachycardia
- inc HR, electircal conduction, contraction
- RENIN RELEASE FROM KIDNEYS ( vasocontrictor or dilator)
**_B2:_**
- bronchodilation
- vasodilation
- stop peristalsis
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which receptor causes tachycardia ?
a1 a2 b1 b2
B1
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which receptor causes dilation (broncho and vaso)?
a1 a2 b1 b2
B2
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which receptor causes bradychardia?
a1 a2 b1 b2 m1 m2 m3 m4
m2
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During epinephrine reversal, what happens to effect of epi? what type of medicine used for epi reversal ?
_Vconstrictor_ effect of epi converted into _vdilator_ effect with **a-blocker** then **B2 vdilator** effect becomes major control
(basically a-blocker cancels out epi a activation effects and only activates B receptors)
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what blocker to give for epi reversal?
a-blocker so that only B receptors active
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DESCRIBE VASOVAGAL REFLEX and CHEMICAL PLAYS ROLE IN IT
ALSO CALLED **VASOGAGUL SYNCOPE**
**NE** activates _baroreceptors_ that stimulate vagal reflex to _reduce HR,_ Leads to opp response to what NE usually does
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WHAT DRUG BLOCKS VASOVAGAL REFLUX (syncope) ?
\*\*
ATROPINE
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IS HUMAN CIRCULATORY SYSTEM OPEN OR CLOSED?
CLOSED
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in circulatory system formula :
what does the pump in a heart tell you?
what does tubing tell you?
what does fluid tell you
pump: **CO**
Tubing: **peripheral resistance (PR)**
fluid: **blood volume (SV)**
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WHAT IS SYSTOLE?
Pressure in arteries when heart contracts
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what is diastole
pressure in arteries when heart relaxes
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WHAT IS **PRELOAD**?
pressure in ventricles _BEFORE_ contraction
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what is afterload?
pressure in arteries against which ventricles must pump (systole)
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side effect of Hydrochlorthiazide ?
HYPOKELEMIA
need K+ supplement
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side effect of spironolactone
HYPERKALEMIA
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WHAT TYPE OF DRUG IS HYDROCHLOROTHIAZIDE (HCTZ)
DIURETIC DRUG (ANTIHYPERTENSIVE) aka water pills
blocks salt reabsorption it then releases more salt when you pee decreasing BP
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spironolactone causes what advere reaction?
hyperkalemia (K+ sparing drug)
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what are vasodilation drugs and what do they do?
**HYDRALAZINE**: opens **_K+_** channels cause vdilation
**CCB**: block **_Ca+_** influx cause vdilation
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WHAT DOES AN **_ACE INHIBITOR_** DO AND WHAT ARE SOME DRUGS? \*\*\*
**BLOCKS** ENZYME CONVERTS ANGIOTENSIN I -\> ANG II (VASOCONTRICOR)
-IPRIL
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WHAT DOES AN ARB DO AND EXAMPLES
**competitive antagonist** at angiotenis II receptor
**- SARTAN**
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MECHANISM OF ACTION FOR LISINOPRIL
ACE INHIBITOR
blocks conversion of angiotensin I -\> II
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LOSARTAN
type of drugmechanism of action
this is a ARB !!!
competitive antagonist: BLOCKS **ANGIOTENSIN II RECEPTOR**
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WHAT ARE ANTIANGINAL DRUGS FOR? WHAT ARE SOME OF THE DRUGS?
FOR I**NSUFFICENT O2 TO CARDIAC MUSCLE** / COMBAT ANGINA
**MONA:**
- morphine
- oxygen
- nitroglycerin
- aspirin
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what type of drugs do you need if heart **fails to pump enough blood**?
Anti-Congestiive Heart failure drugs
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function and mechanism of ANTI CHF drugs and examples
HELP HEART PUMP BLOOD
**_CARDIAC GLYCOSIDES:_**
**block na/k ATPase** to i**ncrease ca+ influx** and promotie positive inotropy in cardiac cells muscles ONLY
\*basically causes induction of na+ which would cause influx of Ca+ that would contract heart \*
**_ACE INHIBITORS:_**
block angiotensin I to II (potent vasoconstrictor)
**DIGOXIN**
**DIGITALIS**
**-PRILS**
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WHAT IS DIGOXIN ?
ANTI CHF DRUG ( caridac glycoside)
block Na/K AtPase to increased ca+ influx promotes inotropy (contraction)
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MAIN FUNCTION OF LISINOPRIL?
**VASODILATOR !!!**
block angio 1 -\> angio II
angio II is a potent vasoconstrictor
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what type of drugs do you give for **irregular heartbeats**?
ANTI-ARRYHTMICS
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MATCH:
Type: 1,2,3,4
na+ blockers for cardiac muscle only
K+ channel blockers
Beta blockers
Ca2+ channel blockers CCB
1- Na+ channel blockers
2- beta blockers
3- K+ blockers
4 - Ca3+ channel blockers
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WHAT IS FUNCTION OF HABBA RECEPTORS?
CAUSE CNS TO GET DEPRESSED
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WHAT ARE DOPAMINE AND SEROTONIC RECEPTORS FCN?
CAUSES CNS TP GET EXCITED
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WHAT TYPE OF DRUGS FOR SCHIZOPHRENICS?
ANTIPSYCHOTICS : schizoz cns system overstimulated need inhibitors
1ST GEN: **DOPAMINE BLOCKER** :
- haloperidol
- phenothiazine
2ND GEN: **DOPAIMINE** AND **SEROTONIN BLOCKER**
- clozapine
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best drug of choice for manic depression ?
LITHIUM
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what are the 3 categories of antidepressants?
what are we trying to increase in antidepressants?
increase **MONAMINES** ( serotonin, dopamine, etc)
1. **SSRI** (slective serotonin reuptake inhibitor)
2. **SNRI/TCA** (serotonin and NE reuptake inhibtor
3. **MAOI** (monamine oxidase inhibtors)
ssri: fluoxetine , citalopram , trazodone
snri: amitriptyline, imipramine
MAOI: phenlzine, tranylcypromine
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WHAT DOES A PATIENT TAKE FOR ANXIETY OR SEDATION ??
ANXYIOLITICS
**BENZOS**
- dizaepam (valium)
- Triazolam
- chlordiazepoxide
-
**BARNITURATES**
- thiopental
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mechanism of action of benzo ?
issue causes ?
inc GABA binding:
- chloride ion influx
- CNS depressed
THROMBOPHLEBITIS (blood clots)
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MECHANISM OF ACTION OF BARBS?
ISSUE WITH BARBS ?
SAME MECHANISM AS BZD
**RESPIRATORY DEPRESSION**
THIOPENTAL **:** quick onseted short duration of action
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Barbs are contraindicated in patients with what illness?
INTERMITTENT PROPHYRIA
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MOST IMPOERTANT FACTOR IN EFFECTS OF GENERAL ANESTHTICS ?
MORE SOLUBLE = MORE POTENT
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WHAT IS DENTAL ANESTHESIA THAT IS USED TO PUT PATIENTS TO SLEEP FOR SURGERY ?
HALOTHANE ?
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WHAT IS HALOTHANE AND A COMPLICATION OF IT?
EXTREMELY POTENT DENTAL ANESTHESIA
**_HEPATOXICITY_** !!!
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PARKINSONS DISEASE:
cause of it?
what drug we use ?
DOPAMINE DEFICIENCY !
* dopamine cant cross BBB but Levodopa **L-dopa** can
* **_CARBIDOPA_** blocks *dopa decarboxylase* allows L-dopa to cross BBB where it is converted to dopamine
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WHAT DRUG DO PARKINSONS PATIENTS TAKE AND WHAT IS MECHANISM?
CARBIDOPA:
blocks DOPA decarboxylase ( causes levodopa to conver to dopamine) allows LDOPA to cross BBB where it is converted to dopamine in brain
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tardive dyskineasia is aneurological side effect of which class of drugs?
1. alcohol
2. tricyclic antidepressants
3. barbs
1. phenothiazine antipsychotics
4. MOAI
**pheno antipsychotics**
involuntary neurological movement disorder caused by the use of dopamine receptor blocking drugs
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which peniccilin only administered by deep IM injections?
1. ampicillin
2. dicloxacillin
3. pen G
4. Pen V
PEN G
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QUINIDINE USED USED TO TREAT:
hypertension
angina pectoris
CHF
supraventricular tacharryhtmia
supraventricular tachyarryhmiia
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a child developes a disease called REYE SYNDROME from what?
ASPIRIN !
(give acetiminophen instead )
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which receptor does oxycodone, morphine, and codeine effect?
Mu-opoid receptors
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which drug is lethal if combines with MAOI ?
MEPERIDINE
