23. Pharmacology: Part 1 (-Anticonvulsants) Flashcards
1
Q
Branch of medicine concerned with the USES, EFFECTS, and MODES OF ACTION of drugs
A
Pharmacology
2
Q
Branch of pharmacology concerned with the EFFECTS OF DRUGS and the MECHANISM of their action (“action of drug on the body”)
A
Pharmacodynamics
3
Q
Branch of pharmacology concerned with the MOVEMENT OF DRUGS within the body (“action of body to the drug”)
A
Pharmacokinetics
4
Q
Pharmacokinetics steps: “ADME”
A
Absorption
Distribution
Metabolism
Excretion
5
Q
Main site of absorption in the body
A
Jejunum of small intestine
6
Q
BQ: Primary solubility of drug to be absorbed?
Form of drug that is EASY TO ABSORB
A
Lipid soluble form
7
Q
Major site of metabolism
A
Liver
8
Q
converts drugs into water soluble form to easily excreted by the kidney
A
Liver
9
Q
Form of drug that is EASY to EXCRETE
A
Water soluble
10
Q
Major site of excretion
A
Kidney
11
Q
Study of drug’s harmful effects
A
Toxicology
12
Q
General rule: Kailan nagiging toxic yung drug?
A
Pag na-“overdose”
13
Q
Has “Adsorption” property (nagsstick sakanya yung toxins; diretso sa excretory system) to prevents ORALLY taken drugs TOXICITY
A
Activated charcoal
14
Q
INDUCES VOMITING (emetic) ; can be used pag nasa GIT pa yung drugs na tinake para di na pumunta sa circulatory system
A
Syrup of Ipecac
15
Q
BQ: It is the “accumulation of drug” because it cannot be excreted by the body?
A
Cumulation
16
Q
“Cumulation” or accumulation of drug in the body is associated with what organ damage?
A
- Liver damage - clearance rate: ⬇️ (marereduce yung nacconvert na Lipid soluble ➡️ WATER soluble)
- Kidney damage - Normal yung liver:nacoconvert yung drug into water soluble BUT hard to excrete!
17
Q
BQ: Drugs contraindicated for GLAUCOMA?
A
Diazepam
Anticholinergic drugs
18
Q
BQ: What is the most common allergenic drug?
A
Penicillin
19
Q
BQ: Drugs SAFE FOR PREGNANCY
A
Local anesthetics : lidocaine
Analgesics : biogesic
Sedative-Hypnotics
*AMOXICILLIN (safe!)
20
Q
BQ: study of DAMAGE TO FETUS during development
A
Teratology
21
Q
Most critical period of development of fetus?
A
1st trimester: organogenesis
22
Q
Examples of Teratogenic drugs
A
- Tetracycline :tooth discoloration (til 8y/o)
- Thalidomide
- An anti cancer drug {no effect sa pregnant rats=no effect ; clinical trial=dysplastic tissues: bata kulang body parts}
23
Q
BQ: study of drug DOSAGE
A
Posology
24
Q
Process of DRUG UPTAKE from the site of administration towards the bloodstream
A
Absorption
25
"Enteral"
Oral
| Rectal
26
"Parenteral" - uses needle
```
IV
IM
Intradermal
Subcutaneous
Intrathecal
```
27
Most common route; easy to administer
Oral route
28
Suppositories
Rectal
29
Route with 100% bioavailability; bypasses the first pass effect; "TOTAL ABSORPTION"
- (100ml inject = 100ml circulatory system)
Intravenous
30
Term: Dose ng drug na nakakarating sa circulatory system
Bioavailability
31
Most common site of IV administration
Antecubital region
32
BQ: Most common muscle used in IM administration
Vastus lateralis
33
Other muscles that can be used in IM administration
1. Gluteus maximus - BQ: ("superolateral"/upper outer corner)
2. Deltoid
34
Used during skin testing to determine if patient has drug allergy
Intradermal
35
Why intradermal during skin test?
Least and slow absorption
36
administration of drug in the SPINAL
Intrathecal
37
Fastest route if the target site is the BRAIN; (sedation)
Inhalational
38
Degree of needle insertion in IV
35 degrees
39
Degree of needle insertion in IM
90 degrees
40
Degree of needle insertion in Intradermal
0 - 15
| {sa boards: piliin yung LOWEST value}
41
Degree of needle insertion in Subcutaneous
45 degrees
42
Most common drug administered subcutaneously
Insulin
43
BQ: Which route bypasses membranes?
Intravenous
| - diretso na sa circulatory system
44
BQ: Which route bypasses ABSORPTION process?
IV
| - distribution na agad
45
Drug properties that influence absorption
Must be "weak acids / weak bases"
- they become MORE LIPID SOLUBLE (mas madali iabsorb sa circulatory system)
*ph of blood = 7.4*
✨ WEAK ACIDS (pH of 6)
- weak acids are attracted to HIGHER pH levels
- 6 ❤️ 7.4
✨ WEAK BASES (ph of 8)
- weak bases are attracted to LOWER pH levels
- 8 💜 7.4
46
Amount of drug that reaches the circulatory system after administration
Bioavailability
47
Synonymous terms to "water soluble" drugs
Hydrophilic
Lipid INSOLUBLE
Ionized
48
Synonymous terms to "lipid soluble"
Fat soluble
Hydrophobic
Water INSOLUBLE
UNionized
49
Drug solubility that is UNABLE to cross the PHOSPHOLIPID bilayer
```
Very hydrophilic (very water soluble)
- hindi makakatagos sa membrane
```
50
Solubility of drug that is UNABLE to be absorb due to INSOLUBILITY IN AQUEOUS FLUID
Very very hydrophobic/lipid soluble
| - insoluble sa aqueous fluid ng intestinal area: hindi nalulusaw sa tubig
51
In reality: What must be the "drug's solubility" to be absorbed?
Drugs must be SLIGHTLY HYDROPHILIC and LARGELY HYDROPHOBIC
| Mej water soluble pero MAS lipid soluble
52
BQ: Primary solubility of drug to be absorbed (sa boards)
Lipid soluble
53
Phenomenon of drug metabolism whereby the CONCENTRATION OF ORALLY TAKEN DRUGS IS REDUCED before reaching the systemic circulation
First pass effect
54
Responsible for First Pass Effect
Liver
| - dadaan muna yung drug sa portal vein to liver(metabolizes drug) bago makarating sa target site
55
Bioavailability is influenced by (3):
Drug solubility
Route
First pass effect
56
Ability of drug to move from circulatory system into their target sites
(- Once na pumasok na sa blood stream)
Distribution
57
Once the pumasok drug sa circulatory system: Meron 2 forms: (active and inactive)
1. Free ionized drug - may effect agad; free floating drug
| 2. Bound drug - reserve; bounded to albumin
58
Most common binding site of drugs?
Albumin
59
Tendency of a substance to separate or dissociate from its binding
Dissociation constant (Kd)
60
Lower Kd ⬇️:
Separation -
Duration of effect -
Onset of action -
Lower Kd ⬇️:
Separation - lesser ⬇️
Duration of effect - longer
Onset of action - slower distribution
61
Higher Kd ⬆️:
Separation -
Duration of effect -
Onset of action -
Higher Kd ⬆️:
Separation - higher ⬆️
Duration of effect - shorter
Onset of action - faster distribution
62
BQ: Most important microsomal enzyme of Liver?
Cytochrome P450
63
FUNCTIONS OF LIVER
1. Lipid soluble to lipid insoluble
- "Water soluble" easily excreted by the kidney
2. Active drug to INACTIVE drug
- detoxification (kasi yung hindi pwdeng magstay na active yung drug: kahit sya yung may effect, toxic pa din)
3. PRODRUGS ➡️ ACTIVE FORM
- prodrug = "inactive drug"
- para maconvert to active need muna mag pass sa LIVER
-
64
Examples of PRODRUGS (inactive drugs=no effect) that must go to the LIVER to be activated:
1. Aspirin (Acetylsalicylic acid) ➡️ Salicylates
2. Codeine ➡️ Morphine
3. Alcohol ➡️ Ethanol
65
2 types of Local anesthesia:
Amide - "ii"
| Ester - "i"
66
Metabolism of Local anesthetics: "EPAL"
Ester - Plasma
| Amide - Liver
67
Most common topical anesthesia?
Benzocaine
68
Exception: dalawang "ii" PERO ester
piPEROcaine
69
Exception: Amide but metabolized in BOTH liver and plasma
Articaine - ("maarti" : metabolized sa liver and plasma)
70
BQ: local anesthesia used if allergic in both ester and amide
```
Diphenhydramine Hcl (Benadryl)
- injected!!
```
71
BQ: Plasma enzyme (metabolism)
Plasma pseudocholinesterase
72
Drugs metabolized in PLASMA
Ester LA
| Succinylcholine
73
BQ: primary use of succinylcholine
For laryngospasm
74
Major organ for excretion
Kidney
75
Drug excreted by the lungs
Nitrous oxide (laughing gas)
76
Drugs or substances excreted by BREAST MILK
Alcohol
Caffeine
Cocaine
Nicotine
77
Time required for a drug to REDUCE HALF of its initial value
Half life (t1/2)
78
Rate at which the active drug is removed from the body
Clearance
79
Amount of drug eliminated is CONSTANT and is NOT DEPENDENT on the CONCENTRATION of drug in plasma fluid
Zero order kinetics
- constant: clearance rate
- not constant: half life
80
Examples of drugs that follow ZERO ORDER KINETICS
Alcohol - (clearance rate=15ml/hr)
Phenytoin
Aspirin
81
Amount of drug eliminated is DEPENDENT on the CONCENTRATION of drug in plasma fluid (most drugs follow this)
First order kinetics
| - may "constant half life"
82
BQ: Which drug has more chances of CUMULATION
a. Zero order kinetics
b. First order kinetics
c. Same
Zero order kinetics: ⬆️ cumulation
( if ⬆️ dose = LONGER to eliminate)
* Sa first order: kahit increase yung dose=may certain time na maeeliminate ung drug (CONSTANT HALF LIFE)
83
Dosage of drug needed to produce an effect
Potency
84
More potent ⬆️
| Dose needed =
⬆️ More potent = ⬇️ dose needed
85
⬇️ Less potent
| Dose needed =
⬇️ potent = ⬆️ dose needed
86
"Potency" of Fentanyl vs Morphine (narcotics: for pain)
Fentanyl (effect: 2-3mcg) MORE POTENT than Morphine (effect: 200-800mcg)
87
Refers to the EFFECT of a DRUG
Efficacy
88
⬆️ Efficacy:
| Efficacious =
⬆️ Efficacy
| ⬆️ MORE efficacious
89
⬇️ Efficacy:
| Efficacious =
⬇️ Efficacy:
| ⬇️ LESS efficacious
90
"Efficacy" of Fentanyl vs Morphine
Fentanyl LESS EFFICACIOUS than Morphine
| Morphine MORE EFFICACIOUS than Fentanyl
91
Maximum effect of a drug where NO EFFECT is added even though DRUG DOSE is INCREASED (Limit)
"Maximal effect" or "Ceiling effect"
| { ⬆️ dose = ⬆️ effect until MAXIMAL EFFECT is reached }
92
BQ: Does doubling the dose, doubles the effect? Yes/No
No - because it will reach "maximal effect": no effect even you add more dose
93
It refers to how well the drug can be used in REAL WORLD
"Effectiveness"
| Drug can have HIGH EFFICACY but ⬇️Effectiveness: "effective pero nakakamatay agad or mas toxic"
94
Dose-Effect ("Dose-Response") Rel:
- The effects of a drug are dose dependent
- (either Therapeutic or Toxic)
* * It can be shown into 2 types of DOSE RESPONSE CURVES:
Graded dose-effect curve
| Quantral Dose-effect curve
95
Curve that describes the Degree of response of a SINGLE BIOLOGICAL UNIT (cell or human) to a given drug dose
Graded Dose-Effect Curve
96
Graded dose effect curve
Y-axis:
X-axis:
Graded dose effect curve
Y-axis: effect
X-axis: dose
97
Curve that describes relationship between the increasing drug dosage and the percentage of POPULATION that shows the drug's pharmacological and lethal effects
Quantal Dose Effect Curve
98
Curve that detects the "MARGIN OF SAFETY" of a drug by comparing the therapeutic dose and toxic dose
Quantal Dose effect curve
99
Quantal Dose effect curve
Y-axis:
X-axis:
Quantal Dose effect curve
Y-axis: Population
X-axis: Dose
100
BQ: Formula of Therapeutic Index
TI = LD50/ED50 ("TLE")
101
BQ: dose of drug that has THERAPEUTIC EFFECT in 50% of population
ED50 ("median EFFECTIVE DOSE")
102
BQ: dose of drug that has LETHAL EFFECTS in 50% of population
LD50 ("median lethal dose")
103
Example of drug that has narrow therapeutic index (drug very lethal)
1. Chemotherapeutic agents
| 2. Digoxine - antihypertensive drug that has VERY NARROW TI
104
Targets of drug action:
1. Receptors
2. Enzymes
3. Drugs acting as Physical or Chemical agents
105
Examples of Drugs with RECEPTORS as target sites:
1. Narcotics
- receptor: mu kappa delta
2. Cholinergic drugs
- receptor: muscarinic
106
Examples of Drugs with ENZYMES as target sites:
1. MAO-Inhbitors
- (Mao breakdown excitatory nt "DoNES")
- MAO-I : "antidepressant" = iniinhbit yung MAO : ⬆️DoNES
2. Anti acetylcholinesterase or Anticholinesterase
- reduce action of "Acetylcholinesterase"
- used to improve muscular contraction
107
BQ: Anti-acetylcholinesterase or Anticholinesterase is used in what disease?
Myasthenia gravis: "muscle weakness"
| - to improve muscular contractions
108
Ability of drug to BIND to its target site
Affinity
| - ("ALL DRUGS have AFFINITY")
109
Ability of drug to produce an EFFECT after binding to its target site
- (kaya niya "iactivate yung receptor")
Intrinsic activity
| - ("NOT ALL can activate receptor/have intinsic activity")
110
Examples of drugs that acts as physical or chemical agents (ginagaya ung sa body)
Epinephrine
| Insulin
111
Part of body where drugs interact to produce their effects
Receptors
112
Drugs that have AFFINITY + INTRINSIC ACTIVITY
Agonists
| - (example: Ach)
113
Drugs that has ✅affinity but no ❌ intrinsic activity (hindi kayang iactivate yung receptor)
Antagonist
114
Elicits a MAXIMAL RESPONSE by activating all or a portion of the receptors
Full agonists
115
Acetylcholine : Agonist/Antagonist?
Ach = Agonist!
- Ach: Parasympathetic
- ✅ Affinity: Nagbbind to sa "muscarinic receptor" ng lahat ng effector organs ng parasympathetic (ex. Lacrimal glands)
- ✅ Intrinsic act: Inaactivate ng Ach yung muscarinic receptor ng lacrimal glands to depolarize para magproduce ng tears
116
Anticholinergic drugs: Agonist/Antagonist?
Antagonists : Anticholinergics
- Belladonna alkaloids (atropine and scopolamine)
- nagaact sa sympathetic NS
- ✅Affinity - nagbbind sa muscarinic receptors
- ❌Int act - doesnt activate receptor
- 📌 Pinaprevent nya lang yung pag bind ng "Ach" sa muscarinic receptor para hindi maactivate!
- 📍 wala tlgang effect sa receptor: Prevents effects of parasympathetics ➡️ ✅sympa effects
117
Anticholinergic drugs: Belladonna alkaloids (2)
Atropine
| Scopolamine
118
What type of antagonist are the anticholinergic drugs (atropine and scopolamine)?
Competitive antagonists
| - nakikipagcompete sa cholinergic drugs
119
Type of antagonist that competes with the receptor of agonists
- which results to decrease POTENCY ⬇️ (dose needed to produce effect)
Competitive antagonists
120
Type of antagonist that has its OWN Receptors; doesnt compete
- results in decrease EFFICACY ⬇️
Non competitive
121
BQ: Naloxone is an ANTAGONIST of what drug?
Narcotics
| - (morphine, codeine, heroin)
122
BQ: Flumazenil is an ANTAGONIST of what drug?
Benzodiazepines
123
BQ: DOC to reverse narcotic effects
Naloxone
| If wala sa choices: go for Naltrexone
124
Intrinsic activity of >0 and <1
- act as antagonist and agonist
- naactivate lng ung receptor partially
- produces LESS maximal response even all receptors are occupied
Partial agonist
125
Theory: Drug effect is proportional to the RATE at which the drug and receptor combine
- (both agonist and antagonist have affinity and intrinsic activity; "immediate binding of drug t receptor dun magkakaeffect then dahan dahan mawawala ung effect")
Paton's Rate Theory
126
Paton's rate theory: Drug associates quickly and disassociates immediately to the receptor, to be able to reassociate again.
Agonists (pag mabilis association and dissociation ng drug)
127
Paton's rate theory: drug associates, but dissociates much SLOWER, therefore REASSOCIATION to the receptor is also SLOWER
Antagonists (pag mabagal dissociation)
128
More accepted drug receptor interaction theories: Clark's or Paton's?
Clark's occupational theory
129
Sedative hypnotics are drugs that are used for:
Sedation - feeling asleep
Hypnosis - sleep
Muscle relaxation
130
Feeling asleep; "loss of anxiety"
Sedation
131
Type of sedation: awake and relax
Minimal or conscious
132
Type of sedation: feeling asleep but can follow commands
Moderate
133
Type of sedation: sleep but can be awaken
Deep sedation
134
"Medically induced coma"
General anesthesia
135
2 classifications of sedative hypnotics
Barbiturates - with Barbaric acid
| Non barbiturates - without
136
Active ingredient of Barbiturates that produces sedative effect
Barbaric acid
137
Barbiturate used to induce general anesthesia
Ultra short acting
- fast induction because "very lipid soluble"
- but rapid recovery
138
Ultra short acting barbiturates
| ultra mura - "TM"
Thiopental
| Methohexital
139
Stage 1 Gen Anes
🔺Anterograde Amnesia (hindi nagfform ng new memories)
| 🔺analgesia (absence of pain)
140
Stage 1 - 4 of General anesthesia by?
Guedel's stages of general anesthesia
141
Type of amnesia na hindi nagfform ng new memories
```
Anterograde amnesia (50 first dates)
- example pag "drunk" = nakakalimot ka
```
142
Type of amnesia na nabubura yung old memories
Retrograde memories (meteor garden)
143
End of stage 1 and Start of stage 2 GA:
Unconscious patient
144
Stage with "delirium"
- very unstable patient: high bp, seizure, etc
- ayaw na ayaw ng anesthesiologist dto kasi madaming complication dito
Stage 2 GA
145
Most stable stage of General anesthesia?
Stage 3 : surgical anesthesia
146
Stage 4 GA:
Stage 4: respiratory depression ➡️ death
147
Kailan umaabot sa stage 4 of GA?
Overdose
148
Used to maintain stage 3 general anesthesia
Long acting barbiturates
149
Where very lipid soluble drugs are stored
Adipocytes
150
BQ: Short acting barbiturates ("SPENT")
Secobarbital
| Pentobarbital
151
BQ: Intermediate acting drugs
| "Kalahati" = "AmBuy"
Amobarbital
| Butabarbital
152
BQ: Long acting barbiturate or sedative hypnotics (pag hndi mo alam, eto na sagot)
Phenobarbital
Mephobarbital
Primidone
153
Type of barbiturate used in insomia
Short acting
| Intermediate acting
154
Type of barbiturate or sedative hypnotic used during epileptic seizures
Long acting
155
BQ: Most commonly used "non barbiturate" in patients
Chloral hydrate (orally)
156
Non barb for insomia
Flumazepam (benzodiazepines)
157
Non barb found in alcohol beverages
Ethanol
158
Classifications of DIPHENHYDRAMINE Hcl
- H1 blocker : anti histamine📌(primary use)
- sedative
- local anes if allergic to amide/ester
- slight anticholinergic effect
159
Regulates "sleep wake cycle" in sedative hypnotics can affect what system
RAS
| Reticular activating system
160
Most common inhibitory nt?
GABA
161
Sedatives vs GABA
Sedatives ENHANCES Gaba
162
Drug Components of lethal injection
Thiopental
Pancuronium bromide
Potassium chloride
163
Primary use of sedative hypnotics?
Sedation
| Induces general anesthesia (ultrashort)
164
BQ: "Any drug that acts on CNS can cause drug dependence" True or False?
True
165
Adverse effect of sedative hypnotics = reddish skin
Stimulates PORPHYRIN PRODUCTION
166
DO NOT COMBINE Sedatives hypnotics with what drugs?
```
CNS depressants: "SNAB"
Sedative hypnotics
Narcotics
Alcohol
Benzodiazepines
```
167
Depressants ("SNAB")
Sedative hypnotics
Narcotics
Alcohol
Benzodiazepines
168
Respiratory depression - death is seen during what stage of general anesthesia
Stage 4
169
Property of CNS depressants (shouldnt be combined because it has excessive effects ⬆️⬆️)
Synergistic (1+1= >2)
170
1+1=0
Antagonistic (cancels effect)
171
1+1=2
Additive
172
BQ: Sedative-Hypnotics produces ANALGESIA. True/False?
Falseeeeeee
173
BQ: Sedative-Hypnotics produces DRUG DEPENDENCE. True/False?
Trueeeee
174
"Anticonvulsants" are aka:
Anti seizure
Anxiolytics
Anti anxiety
Minor tranquilizers
175
Primary use of anticonvulsant drugs
Anti-epileptic or anti seizure
| Antianxiety
176
Type of seizure: abnormal activity in just ONE PART of the brain
Partial seizure
177
Type of seizure: abnormal activity in ALL parts of the brain
Generalized seizure
178
"PETIT MAL"
| - Absence of consciousness; absence of movements for few seconds
Absence seizure
179
Type of Generalized seizure: Awake; muscles are jerking for few seconds to few mins
Myoclonic
180
"Drop seizure"
- Absence of muscle tone
- Awake; muscle relaxation for few seconds to few min
Atonic
181
- most common type of generalized seizure
- Unconscious
- muscle stiffness + jerking movts few mins
Tonic clonic
182
"Grand mal"
Tonic clonic
183
Petit mal
Absence seizure
184
Drop seizure
Atonic seizure
185
"Repeated grand mal" 30mins seizure
Status epilepticus
186
BQ: DOC for tonic clonic seizures and status epilepticus
Diazepam (benzodiazepines)
| Pag wala to sa choices: go for phenytoin
187
BQ: Examples of Calcium Channel Blockers
Nifepidine
| Verapamil
188
Brand name of phenytoin
Dilantin sodium
189
Dental side effect of phenytoin
Gingival hyperplasia
190
Drugs assoc with gingival hyperplasia
Phenytoin
Cyclosporins
Calcium channel blockers (nifedipine / verapamil)
191
Brand name of Carbamazepine
Tegretol
192
BQ: DOC for Tic Douloureux (painful spasms)
Carbamazepine
193
BQ: Common antiseizure drugs (except:)
1. Benzodiazepines (Diazepam)
2. Phenytoin (Dilantin Na)
3. Carbamazepine (Tegretol: Tic douloureux)
BQ: 4. VALPROIC ACID
BQ: 5. Barbiturates (least) - mainly a "sedative hypnotic"
194
Mechanism of action of antiseizure drugs
Potentiates GABA (-) receptors and inhibitory nt
195
Drug uses of anticonvulsants or antiseizure drugs
1. Anti convulsanr or anti seizure or anti epileptics
2. Preoperative sedation (anti anxiety)
3. Induction of Gen Anes
196
BQ: Anticonvulsants used to induce general anesthesia? Which is the most common?
Benzodiazepines
✅ Midazolam : most common; most lipid soluble
📌 Diazepam
❌ Lorazepam : least common; least lipid soluble
197
Primary adverse effect of anticonvulsants
Severe sedation
| *And paradoximal excitement (nakabold hahaha) : "stimulatory effect"
198
Other adverse effects of anticonvulsants
```
✅Severe sedation
✅ Paradoximal excitement
- Drug dependence
- Respiratory depression : stage 4 - overdose
- Drug induced gingival hyperplasia
```
199
BQ: anti-seizure + anti-arrythmic drug
Phenytoin
200
Drug interaction of anticonvulsants
Potentiates other CNS depressants
| wag icocombine bec synergistic 1+1=>2
201
Benzodiazepines are metabolized SLOWLY by the
Liver
202
BQ: active metabolite of benzodiazepines
Dimethyldiazepam
203
BQ: Diazepam is slowly and poorly absorbed in what route of administration?
IM!!
| Diazepam: oral and Iv
204
BQ: Drugs with slight anticholinergic effects ("DiTriBeAM")
```
Diphenhydramine Hcl
Tricyclic antidepressants
Benzodiazepines
Antipsychotic
Meperidine - "Demerol" (narcotic agent)
```
