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SRNAPharmacology I > ANTIHYPERTENSIVES > Flashcards

ANTIHYPERTENSIVES Flashcards

1
Q

Should antihypertensives be stop?

A

Antihypertensive should be given up to the time of surgery

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2
Q

Selective Alpha 2 adrenergic agonists

A

Clonidine (ONLY DISCUSSED )
Dexmedetomine
Methyldopa
Apraclonidine

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3
Q

Selective alpha 2 agonists Properties

A 
Sedation
anxiolytics
Hypnosis
Analgesia
Sympatholysis effects
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4
Q

Selective Alpha 2 adrenergic agonists PROTOTYPE

A

CLONIDINE

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5
Q

CLONIDINE is

A

“CENTRALLY ACTING” selective partial alpha 2 adrenergic receptor agonist.

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6
Q

CLONIDINE alpha 2 to alpha 1 ratio

A

220:1

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7
Q

CLONIDINE also

A

sedative, anxiolytic, and ANALGESIC PROPERTIES (weak)

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8
Q

CLONIDINE is a ______ agent that _______The BBB

A

Lipid soluble

Penetrates

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9
Q

ANESTHESIA clinical use of CLONIDINE

A

Increases the duration of analgesia and reduces dose requirement for narcotic opioid pain medications
Reduces requirements for epidural infusion by 20 % - 60%

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10
Q

ANESTHESIA clinical use of CLONIDINE , and local anesthetics

A

Increases the duration of analgesia, reduce requirement for LOCAL ANESTHETICS

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11
Q

How CLONIDINE works : It prolongs what?

A

Prolongs effects of regional and neuraxial anesthesia via pre and post synaptic alpha 2 receptors

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12
Q

Alpha 2 receptors are both

A

PRE synaptic

POST synaptic

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13
Q

Clonidine ANESTHESIA USED:

A

decrease Requirements of anesthetics *Decrease MAC ) of inhaled and injected anesthetics
Blunt REFLEX TACHYCARDIA associated with tracheal intubation
Decreased fluctuation of BP and HR during anesthesia
AUGMENTS VASOPRESSOR RESPONSE to agents such as IV ephedrine and phenylephrine.

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14
Q

Clonidine for anesthesia can also used if demerol not effective:

A

SHIVERING (75 mcg IV)

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15
Q

The periooperative use reduces the incidence of

A

MI, myocardial ischemia

decrease mortality

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16
Q

ANESTHESIA:: The risk of ______ and risk of ______hemodynamic instability limits the use of clonidine in ______Cases

A

Fetal bradycardia
Maternal
Obstetric

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17
Q

**Most common use of CLONIDINE

A

TREATMENT OF HYPERTENSION

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18
Q

Clonidine can also be used to diagnosis

A

Pheochromocytoma.

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19
Q

ROUTE Of Administration clonidine

A

PO, IV

PACTH, EPIDURAL

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20
Q

Clonidine: Mechanism of action (MAIN)

A

Stimulate inhibitors alpha 2 receptors in the VASOMOTOR CENTER In the brain stem which results in a DECREASE in SNS outflow from this region (BRAINSTEM) to peripheral tissues resulting in
-decreased HR and Myocardiall contractility which decreased CO, peripheral vasodilation

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21
Q

Clonisinw on kidney

A

Decreased renin activity and circulating plasma catecholamine levels.

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22
Q

Clonidine Other mechanism of action

A

Pre synaptic inhibitory alpha 2 receptors in sympathetic peripheral nerve endings resulting in decreased BP and decrease circulating plasma cathecolamines.
COMBINATION of central and peripheral NS effects.

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23
Q

Clonidine antihypertensive effects are caused by a

A

combination of central AND peripheral

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24
Q

EPidurally clonidine produce

A

dose dependent analgesia effects
Because when administered , AGONIZE BOTH PRE AND POST adrenoceptors in the spinal cord .
REDUCES substance P

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25
Clonidine : Mechanism of action on cell membrane.
Modifies function of K+ channels, cells membranes become HYPERPOLARIZED Decrease Aqueous humor and IOP
26
Dexmetomodine (Precedex )does
Same action as CLONIDINE
27
Sympathetic reflexes
Baroreceptor reflexes are blunted by clonidine
28
Clonidine some affinity for peripheral post synaptic | this occur at doses _____that those required to stimulate central ______alpha 2 receptors. seen in
alpha 2 receptors (which can cause vasoconstriction, increased BP) HIGHER; inhibitory; OVERDOSE
29
Pharmacokinetics of CLONIDINE: | Half life? peak hypotensive when?, Lipid soluble? duration? distribution? protein binding?
T 1/2 ~ 12 hours Peak hypotensive 1-3 hours Duration of hypotensive effect after oral dose ~ 8 hours HIGH VOLUME Distribution: HIGLY LIPID SOLUBLE crosses into CNS Protein binding : LOW
30
NOT EVERY LIPOPHILLIC DRUG Is
HIGHLY PROTEIN Bound
31
****Clonidine adverse effects when administered EPIDURALLY and as an INJECTION
BRADYCARDIA | HYPOTENSION
32
CNS side effects of CLONIDINE
Sedation and
33
Clonidine side effects and HYPERTENSIVE
IMPOTENCE
34
Most COMMON side effects of CLONIDINE is
Xerostomia sedation and drowsiness
35
***Adverse effects BLACK BOX FDA EPIDURAL and INJ for CLONIDINE
Not recommended OBSTETRICAL POSTEPARTUM PERI-OPERATIVE pain management RISKS outweighs benefits.
36
****Clonidine withdrawal Syndrome (can be dangerous) caused by ___________ How soon after discontinuation ________ with ____Dose (PO, IV, IM, TD)
Sudden abrupt discontinuation of clonidine may cause withdrawal , 18-36 hours after discontinuation ORAL
37
***Symptoms of clonidine withdrawal syndrome include | Massive ________ _____
Massive sympathetic surge ``` ******REBOUND HYPERTENSION**** Apprehension Nervousness Abdominal pain Sweating Headache ```
38
REBOUND HYPERTENSION risk is increased if oral dose was greater than
1.2mg /day
39
• Treatment of the clonidine induced rebound hypertension _______ 1. Restart clonidine if non-life threatening situation 2. Administer___________ 3. Beta-adrenergic blocking agents (especially nonselective betaadrenergic agents) SHOULD NOT be used alone in this setting, why?
1.urgency of reducing the arterial blood pressure: 2. Administering vasodilators such as ***hydralazine, sodium nitroprusside or a combination of α- and β adrenergic blockade (Labetalol IV) because they may accentuate the rebound hypertension by allowing unopposed α1 adrenergic vasoconstriction caused by activation of the SNS and elevated circulating catecholamines
40
RENIN ANGIONTENSIN-ADOLSERONE SYSTEM
Renin (Juxoglomerular cells) BETA -1 receptors kidney afferent
41
Renin converts | Rate limiting step
Angiotensinogen to Angiotensin 1 (rate limiting step)
42
Renin secretion increased by
Hypotension Decreased renal perfusion Decreased Blood Volume (hemorrhage) Reduction of NA concentration in early distal tubule
43
ACE is a ______Enzymes converting_______
Dipeptidyl peptidase enzyme that converts angiotensin I to angiotensin II Also acts on BRADYKININ , vasodilation substance
44
ACE found in 2 places?
Membrane bound in endothelial cells which line blood vessels | LUNGS
45
Tissues with highest concentration of membrane bound ACE
Lungs
46
Angiotensin II is
POTENT VASOCONTRICTION hormone (more potent than EPI and NE)
47
Angiotensin II binds to ___ ____ ___ receptors
AT1, AT2, AT4
48
Angiotensin II Metabolized to Angiotensin
III, less potent physiologic responses compared to Angiotensin II
49
Angiotensin II can also produced by
non-ACE or Non Ace pathways.
50
Angiotensin II effects mediated via
Angiotensin II binding to AT 1 receptor acts directly on both arteries and veins Stimulated the synthesis & secretion of ALDOSTERONE from adrenal cortex
51
Aldosterone effects.
Increase sodium and water retention | Increase EXCRETION of potassium and hydrogen
52
RAAS Angiotensin II (4 main actions)
Stimulate posterior pituitary gland to secrete ADH Stimulate SNS --> Increase vascular tone Stimulate ALDOSTERONE INHBITS renin release, (once enough has occured)
53
ACE inhibitors available agents
ends in PRIL | Except ENALAPRILAT not enalapril
54
ACE inhibitors mechanism of action
Inhbit ACE conversion angiotensin I to angiotensin II | Prevents angiotensin II mediated vasoconstriction and stimulation
55
Bradykinin levels increases a result of
ACE inhibition
56
BRADYKININ levels are too______leading to 2 main side effects ____ and _______
HIGH: COUGH and angioedema
57
Most ACEI are
prodrugs.
58
ACEI esterified in the liver by
Hepatic Esterases NOT CYP 450 enzymes
59
Only active ACE is
Captopril Lisonopril ENALAPRILAT
60
Which ACEI is the shortest acting ACEI
CAPTOPRIL
61
ACEI clinical effects
dilate arteries and veins by blocking angiotensin II formation and inhibiting BRADYKININ METABOLISM
62
ACEI decreases both
PRELOAD AFTERLOAD Decreased MAP< SBP and DBP
63
ACEI and HR
DO NOT TOUCH HR
64
Clinical Effects continued ACEI
Decreases renal efferent arteriole vasoconstriction | bly blocking angiotensin II formation and angiotensin II
65
ACEI and kidney : Promote renal ______ of _____and ________ by doing what? and by blocking ________ stimulation of ________
Promote renal excretion of sodium and water, by blocking angiotensin II in the kidney and by blocking angiotensin II stimulation of aldosterone secretion
66
For HF ACEI: to vascular
Reduced vascular remodeling
67
ACEi lacks
side effects common with other antihypertensive drugs such as Depression, IMPOTENCE
68
DO Not occur with ACEi
CHF, bronchospasm, bradycardia or PVD | DO NOT CAUSE HYPERGLYCEMIA & HYPOKALEMIA
69
ACEI SIDE effects (Acutely)
1. HYPOTENSION DRY COUGH ***HYPERKALEMIA ***ANGIOEDEMA
70
Drug induced angioedema caused by (leading cause)
ACEi
71
The clinical features of ACEi ANGIOEDEMA are related to what
ELEVATED levels of BRADYKININ
72
Angioedema is life threatening treated with
Epinephrine 0.3-0.5 ml of 1:1000 Solution SC
73
ACEi should NEVER be given to (3 contraindications)
BILATERAL RENAL ARTERY STENOSIS Pregnant Previous angioedema
74
Pre-op management with ACEi
Hypotension | Hemodynamic instability
75
ACEI Inhibitors * NOT IMPORTANT
HTN HF MI LV dysfunction post MI
76
ARB's
Angiotensin II receptor Blocks (ARBs)
77
ARBs blocs which receptor
AT1 Angiotensin II
78
ARBs All ends in
-sartan
79
ARBs MOA short
Selective antagonist of Angiotensin II at the AT1 receptors
80
ARBs mechanism of action
Block and interfered with RAAS by blocking the binding of angiotensin II to the AT 1 receptor on th cell membrane, Thereby inhibitor the action of angiotensin II
81
ARBs
``` Same action of ACEi Decrease vasoconstriction Decrease NE released Decreased ADH and aldosterone release decreased AFTERLOAD AND PRELOAD ```
82
ARBs action
``` Same action of ACEi Decrease vasoconstriction Decrease NE released Decreased ADH and aldosterone release decreased AFTERLOAD AND PRELOAD ```
83
Adverse effects of ARB
HYPERKALEMIA (K* sparring diuretic)'
84
ABRs side effects less incidence of _____
Less incidence of cough and AnGIOEDEMA
85
ARB precautions
Attenuated by NSAIDs.
86
NSAIDS
decrease BP
87
Direct RENIN Inhibitor
Inhibits RAAS first step RENIN
88
ALISKIREN (Tekturna(
The first in a new class of orally effective direct renin inhibitors f or the treatment of HTN
89
Tektruna MOA
Aliskiren works at the first and rate-limiting step of the reninangiotensin-aldosterone system. It binds to the active site of renin and blocks the conversion of angiotensinogen to Ang I, decreasing Ang I levels which subsequently decreases the production of Ang II • Aliskiren is a highly selective, potent competitive inhibitor of renin
90
Adverse effects Aliskiren
Diarrhea HYPERKALEMIA
91
``` DRUGS class affecting RAAS CA-BA-DA ```
``` ACE ARBs Beta BLOCKERS ALDOSTERONE antagonists Direct renin Inhibitors Clonidine ```
92
NEPRILYSIN INHBITOR ______
Sacubitril is a neprilysin inhibitor that acts as an enhancer of the natruiretic peptide neurohormonal pathway
93
Sacubitril is only combined with _______in the brand name product ______ and is only use in _______
Valsartan Entresto Heart failure.
94
Sacubitril MOA ______ rapidly metabolized by _______into active metabolites then inhibits ________ Leads to increased _______ and other vasoactive substances such as _______
Prodrugs rapidly by esterase enzyme into the active metabolite--> inhibits NEPRILYSIN Leads to increase natriuretic petides and other vasoactive substance such as BRADYKININ.
95
Increased levels of bradykinin and the natruiretic peptides results in
Increased level of cGMP, vasodilation (art and veins) Natriuresis, diuresis Suppression of aldosterone
96
SACUBITRIL main adverse effects
HYPOTENSION

SRNAPharmacology I (29 decks)

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