23. Pharmacology: Part 1 (-Anticonvulsants) Flashcards Preview

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1

Branch of medicine concerned with the USES, EFFECTS, and MODES OF ACTION of drugs

Pharmacology

2

Branch of pharmacology concerned with the EFFECTS OF DRUGS and the MECHANISM of their action ("action of drug on the body")

Pharmacodynamics

3

Branch of pharmacology concerned with the MOVEMENT OF DRUGS within the body ("action of body to the drug")

Pharmacokinetics

4

Pharmacokinetics steps: "ADME"

Absorption
Distribution
Metabolism
Excretion

5

Main site of absorption in the body

Jejunum of small intestine

6

BQ: Primary solubility of drug to be absorbed?
(Form of drug that is EASY TO ABSORB)

Lipid soluble form

7

Major site of metabolism

Liver

8

converts drugs into water soluble form to easily excreted by the kidney

Liver

9

Form of drug that is EASY to EXCRETE

Water soluble

10

Major site of excretion

Kidney

11

Study of drug's harmful effects

Toxicology

12

General rule: Kailan nagiging toxic yung drug?

Pag na-"overdose"

13

Has "Adsorption" property (nagsstick sakanya yung toxins; diretso sa excretory system) to prevents ORALLY taken drugs TOXICITY

Activated charcoal

14

INDUCES VOMITING (emetic) ; can be used pag nasa GIT pa yung drugs na tinake para di na pumunta sa circulatory system

Syrup of Ipecac

15

BQ: It is the "accumulation of drug" because it cannot be excreted by the body?

Cumulation

16

"Cumulation" or accumulation of drug in the body is associated with what organ damage?

1. Liver damage - clearance rate: ⬇️ (marereduce yung nacconvert na Lipid soluble ➡️ WATER soluble)

2. Kidney damage - Normal yung liver:nacoconvert yung drug into water soluble BUT hard to excrete!

17

BQ: Drugs contraindicated for GLAUCOMA?

Diazepam
Anticholinergic drugs

18

BQ: What is the most common allergenic drug?

Penicillin

19

BQ: Drugs SAFE FOR PREGNANCY

Local anesthetics : lidocaine
Analgesics : biogesic
Sedative-Hypnotics
*AMOXICILLIN (safe!)

20

BQ: study of DAMAGE TO FETUS during development

Teratology

21

Most critical period of development of fetus?

1st trimester: organogenesis

22

Examples of Teratogenic drugs

1. Tetracycline :tooth discoloration (til 8y/o)
2. Thalidomide
- An anti cancer drug {no effect sa pregnant rats=no effect ; clinical trial=dysplastic tissues: bata kulang body parts}

23

BQ: study of drug DOSAGE

Posology

24

Process of DRUG UPTAKE from the site of administration towards the bloodstream

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)